Drugs

Disease Type
Down's Syndrome Trisomy 21

Edward's Syndrome Trisomy 18
Patau Syndrome Trisomy 13
Turner's Syndrome 45, XO
Klinefelter Syndrome 47, XXY
Fragile X syndrome XLD
Prader-Willi syndrome Disorder of Imprinting
Angelman syndrome Disorder of Imprinting
Cystic Fibrosis (CF) AR
Cri-du-chat syndrome
Di-George syndrome
Neurofibromatosis AD
Huntington's disease AD
Adult Polycystic Kidney disease AD
Ehlers-Danlos syndrome AD
Marfan syndrome AD
Acute Intermittent Porphyria AD
Herediatary Angioedema AD
Von-Willebrands disease AD
Enzyme deficiency/mutation Imp. Clinical findings
Def. of Uroporphyrinogen
C1 esterase inhibitor def.
Drug
Eicosanoids Alprostadil (PGE1)
Eicosanoids Misoprostol (PGE1)
Eicosanoids Dinoprostone (PGE2)
Eicosanoids Carboprost (PGF2a)
Eicosanoids Latanoprost (PGF2a)
Eicosanoids Epoprostenol (PGI2)
Eicosanoids LTB4
Eicosanoids LTA4, LTC4, LTD4
Eicosanoids Zileuton
Eicosanoids Zafirlukast
NSAIDs Aspirin
NSAIDs Ibuprofen
NSAIDs Fenoprofen
NSAIDs Ketoprofen
NSAIDs Naproxen
NSAIDs Oxaprozen
DOC for Gout NSAIDs Indomethacin
NSAIDs Etodolac
NSAIDs Sulindac
NSAIDs Piroxicam
NSAIDs Meloxicam
NSAIDs Ketorolac
NSAIDs Diclofenac
NSAIDs Nabumetone
NSAIDs Diflunisal
NSAIDs Celecoxib
NSAIDs Valdecoxib
NSAIDs Rofecoxib
NSAIDs Acetaminophen
Gout Colchicine
Chr. Gout Allopurinol
Chr. Gout Probenecid
Chr. Gout Sulfinpyrazone
Chr. Gout Febuxostat
Anti Histamine Diphenhydramine (Benadryl)

Anti Histamine Dimenhydrinate (Dramamine)
Anti Histamine Promethazine (Phenergan)
Anti Histamine Hydroxyzine (Atarax)
Anti Histamine Chlorpheniramine (Teldrin)
Anti Histamine Cyclizine (Marezine)
Anti Histamine Meclizine (Antivert)
Anti Histamine Cyproheptadine (Periactin)
Anti Histamine Cetirizine (Zyrtec)
Anti Histamine Loratadine (Claritin)
Anti Histamine Desloratadin
Anti Histamine Astemizole
Anti Histamine Fexofenadine (Allegra)
Anti Histamine Azelastine (Astelin)
Anti Histamine Acrivastine
Type MoA
Salicyclic acid Irreversible Inactivates COX; Forms irreversible covalent bonds w/

Propionic acid Reversible non-selective COX inhibitors
Propionic acid Inhibits synthesis of PGs
Acetic acid
Acetic acid
Oxicam
Oxicam relatively COX-2 inhibitor at therapeutic dose
used parenterally (IV or IM)
COX-2 selective inhibition

Inhibitis COX in CNS; peripheral blocking of pain impulses in PNS
Binds to intracellular protein tubulin-> dec. microtubular polymerization-> inhibit leukocyte m

Inhibit of uric acid(Comp. inhibit. of last 2 steps in uric acid biosynthesis)
Inhibit. Prox. Tubular reabsorption of urate, inhibit secretion of acidic drugs
Inhibit. Prox. Tubular reabsorption of urate, inhibit secretion of acidic drugs
Non-purine, potent & selective inhibitor of Xanthine oxidase
1st gen Antihistamine

1st gen Antihistamine Stronger sedative effects
2nd gen Antihistamine
Effect
vasodilation in male impotence
Protection of Gastric mucosa; Uterine contractions
Uterine SM contractions; used for cervical ripening; also as an abortifacient (w/ Mifepriostone)
Uterine and Bronchial SM contractions (used as abortifacients w/ Mifepristone)
Decrease Intraocular pressure
Platelet stabilizer and vasodilator
Inflammatory mediator; Neutrophil chemoattractant; Inc. free radical formation
Anaphylaxis and Bronchoconstriction (role in asthma)
Inhibits Lipoxygenase pathway
LT-receptor antagonists
Anti-Platelet (60-160mg); Analgesic & Anti-pyretic (650-1000mg); Anti-inflammatory (3-6g); Hyperventilation & Resp. Alkal
Analgesic, Antipyretic, anti-inflammatory
Potent anti-inflammatory, anti-pyretic, analgesic
Anti-pyretic (CNS);Weak Anti-inflammatory
ular polymerization-> inhibit leukocyte migration & phagocytosis

acid biosynthesis)
cretion of acidic drugs
cretion of acidic drugs
Used for (Tx)
Maintainance of PDA
Tx of NSAID induced ulcers
an abortifacient (w/ Mifepriostone)
nts w/ Mifepristone)
Tx of Glaucoma
Tx of Primary Pulmonary HTN
ree radical formation
Role in asthma
used in Tx of Asthma
used in Tx of Asthma
00mg); Anti-inflammatory (3-6g); Hyperventilation & Resp. Alkalosis (6-10g); Dehy
Tx of Arthritis
Tx of Acute Gouty arthritis, Ankylosing spondylitis, closure of PDA, Thromocytopenia, Aplastic anemia
Tx of Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis

Tx of Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis
Tx of Oosteoarthritis & Rheumatoid arthritis

Toxicity Tx for Toxicity
Contraindicated in Pregnancy
Hyperuricemia; Uricosuria; Gastritis, ulcers, HSR, Gastric Lavage; HCO3 (IV)
of PDA, Thromocytopenia, Aplastic anemia
Cross allergic w/ Sulfonamides; HTN

risks for MI, Stroke; HTN
Risks for Toxic epidermal necrolysis, Steven-Johnson syndrome, Erythema Multiforme; HTN
Hepatic toxicity; Renal tubular necrosis (NAPQ1) N-acetylcysteine; admin. of activated charcoal
Diarrhea, N/V, abd. pain; Hepatic necrosis, Acu. Renal fail., seizures, hair loss, bone marrow suppression
GI distress, Peripheral neuropathy, Rash, Vasculitis, Stone formation
GI distress, Rash, Nephritic syn., Crystallization
Drug
Eicosanoids Alprostadil (PGE1)
Eicosanoids Misoprostol (PGE1)
Eicosanoids Dinoprostone (PGE2)
Eicosanoids Carboprost (PGF2a)

Eicosanoids Latanoprost (PGF2a)
Eicosanoids Epoprostenol (PGI2)
Eicosanoids LTB4
Eicosanoids LTA4, LTC4, LTD4

Eicosanoids Zileuton
Eicosanoids Zafirlukast
Effect Used for (Tx)
vasodilation in male impotence Maintainance of PDA
Protection of Gastric mucosa; Uterine contractions Tx of NSAID induced ulcers
Uterine SM contractions; used for cervical ripening; also as an

abortifacient (with Mifepriostone)
Uterine and Bronchial SM contractions (used as abortifacients
will Mifepristone)
Decrease Intraocular pressure Tx of Glaucoma
Platelet stabilizer and vasodilator Tx of Primary Pulmonary HTN
Inflammatory mediator; Neutrophil chemoattractant; Inc. free
radical formation
Anaphylaxis and Bronchoconstriction (role in asthma) Role in asthma
Inhibits Lipoxygenase pathway used in Tx of Asthma
LT-receptor antagonists used in Tx of Asthma
Toxicity/Side effects
Contraindicated in Pregnancy
Drug Type MoA
Irreversible Inactivates COX; Forms
NSAIDs Aspirin Salicyclic acid irreversible covalent bonds w/
Platelets via acetylation
Reversible non-selective COX

NSAIDs Ibuprofen Propionic acid
inhibitors (RNSCIs)
NSAIDs Fenoprofen Propionic acid RNSCIs
NSAIDs Ketoprofen Propionic acid RNSCIs
NSAIDs Naproxen Propionic acid RNSCIs
NSAIDs Oxaprozen Propionic acid RNSCIs
NSAIDs Indomethacin Propionic acid Inhibits synthesis of PGs
NSAIDs Etodolac Acetic acid

NSAIDs Sulindac Acetic acid
NSAIDs Piroxicam Oxicam
relatively COX-2 inhibitor at

NSAIDs Meloxicam Oxicam therapeutic dose
NSAIDs Ketorolac used parenterally (IV or IM)

NSAIDs Diclofenac
NSAIDs Nabumetone
NSAIDs Diflunisal
NSAIDs Celecoxib COX-2 selective inhibition
NSAIDs Valdecoxib COX-2 selective inhibition
NSAIDs Rofecoxib COX-2 selective inhibition
Inhibitis COX in CNS; peripheral

NSAIDs Acetaminophen
blocking of pain impulses in PNS
Effect Used for (Tx) Toxicity
Anti-Platelet (60-160mg); Analgesic & Anti-pyretic
Hyperuricemia; Uricosuria;
(650-1000mg); Anti-inflammatory (3-6g);
Gastritis, ulcers, HSR, Reye's
Hyperventilation & Resp. Alkalosis (6-10g);
syndrome, Hepatotoxicity
Dehyadration & Met. Acidosis (10-20g)

Tx of Arthritis
Tx of Acute Gouty arthritis,

Ankylosing spondylitis,
closure of PDA,
Thromocytopenia, Aplastic
anemia
Tx of Rheumatoid arthritis,
osteoarthritis, ankylosing
spondylitis
Tx of Rheumatoid arthritis,
osteoarthritis, ankylosing
spondylitis
Tx of Oosteoarthritis & Cross allergic w/

Potent anti-inflammatory, anti-pyretic, analgesic
Rheumatoid arthritis Sulfonamides; HTN
risks for MI, Stroke; HTN
Risks for Toxic epidermal

necrolysis, Steven-Johnson
syndrome, Erythema
Multiforme; HTN
Hepatic toxicity; Renal tubular

Anti-pyretic (CNS);Weak Anti-inflammatory
necrosis (NAPQ1)
Tx for Toxicity
N-acetylcysteine; admin. of
activated charcoal
Drug
Gout Colchicine
Chr. Gout Allopurinol
Chr. Gout Probenecid
Chr. Gout Sulfinpyrazone
Chr. Gout Febuxostat

MoA
Binds to intracellular protein tubulin-> dec. microtubular
polymerization-> inhibit leukocyte migration & phagocytosis
Inhibit of uric acid(Comp. inhibit. of last 2 steps in uric acid
biosynthesis)
Inhibit. Prox. Tubular reabsorption of urate, inhibit secretion of
acidic drugs
Inhibit. Prox. Tubular reabsorption of urate, inhibit secretion of
acidic drugs
Non-purine, potent & selective inhibitor of Xanthine oxidase

Toxicity
Diarrhea, N/V, abd. pain; Hepatic necrosis, Acu. Renal fail.,
seizures, hair loss, bone marrow suppression
GI distress, Peripheral neuropathy, Rash, Vasculitis, Stone
formation

Drug Type
Anti Histamine Diphenhydramine (Benadryl) 1st gen Antihistamine
Anti Histamine Dimenhydrinate (Dramamine) 1st gen Antihistamine
Anti Histamine Promethazine (Phenergan) 1st gen Antihistamine
Anti Histamine Hydroxyzine (Atarax) 1st gen Antihistamine
Anti Histamine Chlorpheniramine (Teldrin) 1st gen Antihistamine
Anti Histamine Cyclizine (Marezine) 1st gen Antihistamine

Anti Histamine Meclizine (Antivert) 1st gen Antihistamine
Anti Histamine Cyproheptadine (Periactin) 1st gen Antihistamine
Anti Histamine Cetirizine (Zyrtec) 2nd gen Antihistamine
Anti Histamine Loratadine (Claritin) 2nd gen Antihistamine
Anti Histamine Desloratadin 2nd gen Antihistamine
Anti Histamine Astemizole 2nd gen Antihistamine
Anti Histamine Fexofenadine (Allegra) 2nd gen Antihistamine
Anti Histamine Azelastine (Astelin) 2nd gen Antihistamine
Anti Histamine Acrivastine 2nd gen Antihistamine
MoA Effect Used for (Tx)
Stronger sedative effects

Sedation, antinausea, antiemetic,
blocks Autonomic receptors antiparkinsonism, anticholinergic,
block H1 receptors serotonin blocking action, Allergic
reactions: hay fever, rhinitis,
urticaria
Preoperative sedation
Sleep aids and cold medications,
motion sickness, vertigo, N and V
of pregnancy
NO or less sedative effect

Antiallergic, loratidine has
anticholinergic effects
Drug Type Other
serotonin Buspirone partial agonist of 5HT1A
serotonin Sumatriptan agonist of 5HT 1D
serotonin Olanzapine antagonist of 5HT 2A (atypical

antipsychotic
serotonin Cyprohepatidine antagonist of 5HT 2 H1 blocking action
serotonin Ondansetron antagonist of 5HT 3

serotonin Cisapride receptor activator of 5HT 4
Uterine smooth muscle
Ergot Ergonovine
contraction
partial agonist of 5HT2 and alpha Constriction of cerebral
Ergot Ergotamine adrenoreceptors vessels
partial agonist of 5HT2 and alpha
Ergot Methysergide
adrenoreceptors
Used for (Tx) Tx for Toxicity
Generalized anxiety disorder
Migraine headaches
Decrease negative symptoms of psychosis
Carcinoid syndrome, GI tumors

decrease emesis in chemotherapy, radiation and post
operatives
Cardiac k channel blocker
Control of late uterine bleeding after placental Never be given
delivery before delivery
Prodrome for migraine attacks
Prophylatic in migraine, used ass substitute for LSD

Duration of action Agent
Alprazolam
Triazolam
Short <12 hrs
Oxazepam
Midazolam
Temazepam
Intermediate 12- 24 hrs
Lormetazepam
Lorazepam (Of all long acting it
has shortest half life.)
Diazepam
Clonazepam
Chlordiazepoxide
Long > 24 hrs
Tetrazepam
Non BZs MOA

Zolpidem, Zalephlon Activate BZ1 receptors
Buspiron 5HT1a partial agonist

Eszopiclone Non BZ
Indications
Procedural sedation
Anesthesia induction
Sleep onset insomnia
Sleep-onset as well as sleep maintenance insomnia
Anxiety Disorder
Anxiety and panic attacks, IV in status epilepticus
Stress Disorders
Night trerrors
Ecclampsia
Acute episodes of paranoia
Muscle relaxation
Status Epilepticus
Alcohol Withdrawal Syndrome
Characteristics
Used in sleep disorders. Effect reversed by Flumazenil
Non sedating, indicated for generalized anxiety

disorders. Takes 1 to 2 weeks for effect.
Used in treatment of insomnia
Potential for depen.
Very high
High to very high
High
Duration of action Pharmacological agent
Methohexital
Ultra-short (15 minutes–3
hours) Thiopental
Pentobarbital
Short (3–6 hours)
Secobarbital
Amobarbital
Intermediate (6–12 hours)
Butalbital
Phenobarbital
Long (12–24 hours)
Primidone
Indications
General anesthesia (see intravenous anesthetics)
Status epilepticus
Reduction of intracranial pressure for brain
edema following trauma or surgery
Sedation for electroconvulsive therapy (methohexital)
Preanesthetic sedation
Short-term treatment of insomnia
Tension-type headache
Generalized-onset and focal-

onset seizures (see anticonvulsant drugs)
Status epilepticus
Neonatal seizures
Ethanol withdrawal
Preanesthetic sedation
Gilbert syndrome (to reduce hyperbilirubinemia)
Generalized-onset and focal-onset seizures
Essential tremor
Drug Action
Dislfiram Inhibit aldehyde dehydrogenase
Long acting opiod receptor

Naltrexone antagonist
Weak NMDA receptor antagonist

Acamprosate and GABAa receptor activator
Fomipezole Inhibit alcohol dehydrogenase
FOMEpizole: For Overdosing on Methanol or Ethylene glycol!
It is DISgusting to drink alcohol when taking DISulfiram!

Effect Used for tx
Treatment for alcohol use
Stop further metabolism acetaldehyde accumulates disorder
Reduce craving for alcohol and rate of relapse to

either drinking or alcohol dependence
Reduce short term and long term relapse rate when

combined with psychotherapy
Treatment for methanol or

ethylene glycol poisoning
ethanol or Ethylene glycol!
hen taking DISulfiram!
Causes
Symptoms in one who drink alcohol Flushing, throbbing
headache, N/V, sweating, Hypotension and confusions
Cause dose dependent hepato toxicity

Drug Action
Nitrous oxide Rapid onset and

recovery.
Desflurane Very rapid onset and

recovery
Sevoflurane Rapid onset and

recovery.
Relatively slow onset

Isoflurane
and recovery.
Medium speed of
Enflurane
onset and recovery
Halothane Medium speed of

onset and recovery
System
Cardiovascular
Respiratory
Brain
Kidney
Liver
Specific characteristics
Usually insufficient if used alone → often combined with a more potent
inhalational anesthetic to achieve the “second gas effect”.
Pungent odor; irritates airways → not suitable for induction of anesthesia,

coughing and laryngospasm.
Most commonly used inhalational anesthetic. Non-pungent → suitable for

induction of anesthesia
Most potent of the fluranes. Does not provoke seizures and preffered for
neurosurgery. Pungent odor → not suitable for induction of anesthesia
Does not sensitize heart catecholeamines, non irritating, seizures occur at

deeper levels.
Sensitize heart to catecholamines, Inhibit uterine and intestinal
contractions. Bronchus Dilates so preffered in asthma.
Effects
Myocardial depression leading to decrease output
All except nitrous oxide are respirtory depressants, they all decrease tidal
volume and cause hypercapnia, suppression of mucous cilliary clearence which
may predispose to post operative analyxis
Flourinated anesthetics decrease vascular resistance and lead to increase in

cereebral blood flow which lead to increase in intracranial pressure.
Decrease glomerular filtration rate increase renal vascular resistance and

decreased renal plasma flow.
Fluorinated anesthetics decreased hepatic blood flow.
Side effects
Chronic exposure causes megaloblastic anemia
Caution in renal failure, contraindicated in

epileptics
Causes Hepatotoxicity (hepatitis) and
malingnant hyperthermia
Indication
Total intravenous anesthesia (TIVA) drug of choice, Sedation
Propofol in ICU, Short procedures, Rapid induction.
IV anesthesia for patients with hemodynamic instability,

Etomidate adrenocortical suppression
Ideal emergency anesthesia for polytrauma patients, Short

Ketamine painful procedures (e.g., fracture reduction), Treatment-
resistant asthma
Barbiturates(thiopental a IV anesthesia induction (esp., short procedures, risk of

nd methohexital) raised intracranial pressure)
Opioids (e.g., fentanyl, m Analgesia during induction and/or maintenance anesthesia

orphine)
Benzodiazepines (e.g., mi IV anesthesia induction, Short outpatient procedures,
dazolam) Preoperative sedation and Endoscopy
Action Side effects
Antiemetic, No analgesic or muscle relaxant effects, Hypotension. Pain at site of injection is most
Very rapid onset and recovery. 45 sec to 15 min common adverse effect.
↓ Intracranial pressure, little to no effect on the cardiovascular and

_
respiratory system. Rapid onset and duration of action. 5 to 10 min
Sympathomimetic effects, ↑ Intracranial pressure, Dissociative

anesthesia, Psychotomimetic effects motor restless and rigidity _
more common
Respiratory depression, ↓ Intracranial pressure,

_
Antiepileptic effects and Cytochrome P450 induction
Muscle rigidity, Cardiovascular and respiratory depression.

Neuroleptic anesthesia (fentanyl). _
↓ Blood pressure, Anterograde amnesia, Neuroleptic anesthesia

[midazolam, Droperidol(long acting)]. _
Drugs Duration
Procaine Short
Chloroprocaine Short
Lidocaine Intermediate
Prilocaine Intermediate
Bupivacaine Long cardiotoxicity
Ropivacaine Long
Drug Name Increase GABA Decrease sodium
Block Na+ channels in

Phenytoin _
their inactivated state
Carbamazepine _ Inactivates Na+ channels
Increase duration of GABA

Phenobarbital channels Block Na+ channels
Ethosuximide _ _
Valproic acid Inhibit GABA transaminase Block Na+ channels
Benzodiazepines Indirect GABAa agonist _
Lamotrigine _ Block Na+ channels
Felbamate _ Block Na+ channels
Gabapentin Increase GABA effect _
Tiagabine Blocks GABA transporters _
Topiramate Increase GABA effect Block Na+ channels

Vigabatrin Inhibit GABA transaminase _
Adverse Effects Drugs causing Symptoms
Hepatotoxicity Valproic acid Abdominal pain, fever and

chills, N/V.
Mid epigastric sharp pain

Pancreatitis Valproic acid
radiating towards back.
Pallor, weakness,
Aplastic anemia Felbamate
fatigue,fever.
Steven-johnson Lamotrigine Fever and widespread skin
syndrome pain
Megaloblastic Pallor, weakness,

Phenytoin, phenobarbital
anemia fatigue,fever.
Peripherial Phenytoin Hearing loss, burning

Neuropathy sensations, weakness.
Pain while urinating, lower

Kidney stones Topiramate back pain, polyuria, loss of
appetite
Blurr vision, frontal

Glaucoma Topiramate
headache, vision loss.
Decrease calcium Decrease Glutamic acid
_ _
_ _
_ _
Block T-type calcium ion _

current in thalamic neurons
Block T-type calcium ion Decrease neuronal excitability

channels
_ _
_ Block Glutamate receptors
Block T-type Calcium

Block Glutamate NMDA receptors
channels
Inhibit Ca2+ T and L type
channels in thalamic _
neurons
_ _
_ Block Glutamate AMPA receptors
_ _
Risk factors or Imp points in

patient history Any Imp Findings
Use of anti convulsants and Elevation of liver enzymes

their dose
Use of anti convulsants and
Elevation of serum lipase and
their dose and history of
amylase.
alcohol abuse
Petechiae, easy bruising, bleeding,

neutropenia followed by
their dose.
thrombocytopenia.
their dose. Immunosupressed Erythromatous/pupuric macules,
shedding of skin.
and family history.

Deficient levels of Vitamin B12 and B9.
their dose and diet of patient.
Use of anti convulsants and Deficient levels of Vitamin B1.

their dose.

X-ray of kidneys, increase urea,
their dose. Diet containing
creatinine and calcium.
calcium.

Fundoscopy showing cupping and
their dose, history of diabetes pallor of optic disc.
mellitus, myopia.
Other actions or specific details to
mention
Induces CYP450
Used in general tonic clonic seizures, partial
seizures and bipolar disorder
Induces CYP450 and does autoinduction. Also

used as DOC in trigeminal neuralgia
Selective antiseizure activity at low doses
Only used in absence seizures
Inhibits CYP450
First line treatment for Status epilepticus

First line treatment for focal seizures, toxicity
causes steven johnsons syndrome.
Used in Lennox Gastaut syndrome
Used in neuropathic pain, migraine
Toxicity causes flu like symptoms

Used in Migraine prophylaxis
Used for refractory Focal seizures.
Drugs Type
D- Tubocurarine (longer Nicotinic receptor antagonist.(non

half life > 60mins) depolarizing and competitive)
Pancuronium (longer half Nicotinic receptor antagonist.(non

life > 60mins) depolarizing and competitive)
Atracurium (intermediate Nicotinic receptor antagonist.(non

acting) depolarizing and competitive)
Nicotinic receptor antagonist.(non

Mivacurium
depolarizing and competitive)
Succinylcholine Nicotinic receptor agonist.(depolarizing

and non-competitive)
Tizanidine Spasmolytics
Dantrolene Spasmolytics
Benzodiazepines
Spasmolytics
(diazepam)
Baclofen Spasmolytics
MOA Other
Dimnish frequency of opening of Na+
channels so no depolarization, Block
Implicated in Malignant hyperthermia
ANS ganglia and release histamine
decrease BP.
Dimnish frequency of opening of Na+ Increases BP vagolytic and

channels so no depolarization. Sympathomimetic
Dimnish frequency of opening of Na+

Safe in hepatic or renal dysfunction.
channels so no depolarization.
Dimnish frequency of opening of Na+ Metabolized by plasma

channels so no depolarization. pseudocholinesterase: histamine release.
Short duration due to fast inactivation by

Phase I: Depolarizing. Phase II: pseudocholinesterase and genotypic
Desensitizing. variants with low enzyme activity which
cause prolong effects.
Alpha-2-agonist, congener of clonidine. Effective as diazepam but cause less

sedation.
Block activator Ca release from SR by

binding on RyR1 receptors and block Used in treatment of malignant
hyperthermia.
opening of channel.
Facillitate GABA at GABAa receptors. Sedation and reduce muscle tone.
Facillitate GABA at GABAb receptors in Effective as diazepam but cause less

spinal cord. sedation.
Side effects
Bronchial secretion and

bronchiospasm
Break down product

Laudanosine causes seizures.
Malingnant Hyperthermia
Drowsiness, hypotension, dry

mouth, asthenia.
Class Drug MOA
Odansetron Competitively block 5HTs
Granisetron receptors, prevent both central and
Serotonin 5HT3 Antagonist
Dolasetron peripheral stimulation of vomiting
Palonosetron centers
Neurokinin receptor antagonist (NK- Aprepitant (oral)

Central blockade in area postrema
1) Fosaprepitant (IV)
Prochloroperazine Inhibition of dopamine and

Phenothiazines (Antipsychotics) Promethazine muscuranic receptors, central
Thiethylperazine effect on area postrema
Butyrophenons (Antipsychotics) Droperidol Central dopaminergic blockade

Haloperidol
Methoclopramide
Substituted Benzamines Dopamine receptor blockade
Trimethobenzamide
Diphenhyramine
Dimenhydrinate Block H1 receptors (antagonists)
H1 Antihistamines
Meclizine Block H1 receptors (antagonists)
Anticholinergic agent Hyoscine (scopolamine) Muscuranic receptor antagonist
Lorazepam
Benzodiazepine GABA agonists
Diazepam
CB1 agonist as this are GI coupled

Cannabanoids Dronabinaol
they are inhibitory to vomiting
Clinical Use Side effects.
Action is restricted to emesis attributable to vagal Headache, dizziness, constipation, QT prolongation
stimulation and chemotherapy (dolasetron), Anaphlactoid reaction include
Post operative is odan and dolasetron angioedema, hypotension, urticaria, bronchospasm
Post radiation is odan and granisetron (odansetron)
Fatigue, dizziness, diarrhea, decrease INR

Combination therapy with 5HT anta. and
(international normalised ratio) in patients taking
corticosteroids to prevent acute and delayed N/V
warfarin, may inhibit metabolism of drugs
after emetogenic cancer chemo
metabolized by CYP3A4
Diarrhea, depression, restlessness, drowsiness, OD

Antiemetic, antihistamine, antipsychotic, leads to reversible extrapyramidal syndrome
anticholinergic and sedative effects. (dystonia, tardive dyskinesia, parkinsonism,
akathasia)
Mood disorders, Antiemetic and used as an _

adjunct in anesthesia (Droperidol)
Prokinetic effect to treat diabetic and post surgery OD leads to reversible extrapyramidal syndrome
(dystonia, tardive dyskinesia, akathisia
gastroparesis, persistant GERD pseudoparkinsonism)
Significant anticholinergic properties, Strong

sedative and antiemetic for vestibular causes Drowsiness, confusion, anticholinergic side effects
(midriasis, tachycardia, dry mouth, urinary retention)
Minimal anticholinergic and less sedative
Anticholinergic side effects (midriasis, tachycardia,

Prevention of motion sickness dry mouth, urinary retention)
Used before chemotherapy to reduce anticipatory

Sedation
vomiting or vomiting caused by anxiety.
Appetite stimulant in AIDS patients and antiemetic

used in chemo induced emesis (severe) when Dizziness, drowsiness, confusion
conventional antiemetic fail
Class Drug MOA
Amitriptyline
Imipramine Block reuptake of both NE and 5HT
Clomipramine
Tricyclic antidepressants (TCAs) Desipramine

Block reuptake of NE additional effects like M
Nortriptyline
block, alpha-1-block, histamine-1-block,
Amoxapine
sedation, decrease seizure threshold, greater
Maprotilline
cardiotoxicity (OD)
Atomoxetine
Inhibit both MAO type A (metabolize

Phenelzine
catecholamines, serotonin and tyramine in
MAO inhibitors (MAOIs) Tranylcypromine
intestine and other tissue) and MAO type B
Selegiline
( Metabolize dopamine in brain and platelets)
Fluoxetine
Fluvoxamine
Selective serotonin reuptake Selectively block reuptake of 5HT which
Paroxetine
inhibitors (SSRIs) increase serotonergic neurotransmission
Sertraline
Citalopram
Amoxapine
Block NE reuptake
Maprotiline
Nefazodone Block 5HT reuptake, P450 inhibitor
Tradozone (nefazodone)
Heterocyclic antidepressants Block pre synaptic alpha 2 receptors prevent

Mirtazapine feedback inhibition of transmitter release,
increase neuronal release of NE and Serotonin
Minimal effects on NE but may affect dopamine

Bupropion
transmission
Mood Stabilizer Lithium Inhibits inositolmonophosphatase, decrease

PIP2 and cAMP
Serotonin Norepinephrine 5HT and NE reuptake inhibition does not block

Venalfaxine
reuptake inhibitor Muscuranic, adrenergic or histamine receptors.
Clinical Use Side effects.
Major depressive disorder Antimuscuranic- dry mouth, metallic taste,

tachycardia, urinary retention, arrhythmias
Phobic and panic anxiety states
Neuropathic pain (amitriptyline) Hypotension
Seizures
Enuresis (imipramine)
Excessive excitation
Obsessive compulsive disorder
Weight gain, Withdrawal - N/V, headache,
(clomipramine) vertigo, malaise, nightmares.
Anticholinergic Symptoms
In Atypical depressions but
Orthosthatic hypotension
infrequent.
Weight gain
Anxiety Withdrawal: Headache, nausea,

Major depression
Insomnia vertigo- malaise
Anxiety States- panic, phobia, social
Agitation
Pre menstrual syndrome (PMS)
Bruxism (grinding of teeth)
Bulimia
Sexual dysfunction (anorgasmia,
OCD
impotence,etc.), Seizures (OD)
Alcoholism
Weight loss.
Anxiety
Drowziness, dry mouth , constipation
Depression
Cause sedation and priapism Erectile dysfunction, headache, dry
(prolong erection of penis) mouth,dizziness.
Potent antihistamine with greater Drowziness

sedating effects, also elevate hepatic Dry mouth
level in cases of agranulocytosis Constipation
Drowziness
Used for smoking cessation Dry mouth
Constipation
DOC for Bipolar affective disorder, Tremor, ataxia, choreoathetosis, acne, edema, visual dysfunctions, seizures, goiter,
need antidepre. for depressive hypothyroidism via inhib. Of 5' deiodinase, nephrogenic Diabe.Insi. via uncoupl.
phases and sedatives for manic Vassopressin V2 receptors, neonatal toxicity- cyanosis, lethargy, possible hepatomegaly,
phase teratogenicity no drug interactions.
Drug interactions
Hyperthermia, seizures, coma, and death

with MAOIs
Serotonin syndrome with selective
reuptake inhibitors
Hypertensive crisis with tyramine, NE

Olmesartan is used to
uptake blockers, alpha agonists and L-
treat high blood
dopa, hyperthermia, HTN, seizures,
pressure
serotonin syndrome with SSRI
Serotonin syndrome
Diaphoresis
Rigidity
Myoclonus
Hyperthrmia
ANS instability
Seizures
ne, edema, visual dysfunctions, seizures, goiter,

dinase, nephrogenic Diabe.Insi. via uncoupl.
l toxicity- cyanosis, lethargy, possible hepatomegaly,
Class Agents Mechanism of action
Haloperidol
Typical Fluephenazine
High potency Perphenazine
antipsychotics Trifluoperazine
Pimozide
Block D2 receptors in
mesolimbic pathways
Chlopromazine
Low potency Thioridazine
Promethazine
Clonazapine
Olanzapine
Risperidone
Quetiapine
Atypical Amisulpride
Ziprasidone Block 5HT 2 receptors and D2
Antipsychotics Aripiprazole
receptors
Lurasidone
Asenapine
Iioperidone
Paliperidone
Indications Side effects
Hyperprolactinemia,
Extrapyramidal effects :-
Alleviate the positive psuedoparkinsonism, Acute
symptoms of psychosis
dystonia, Akinesia, akathisia,
Pimizode/Haloperidol is DOC Tardive dyskinesia, Neuroleptic
for tourette's Syndrome and
in initial treatment of bipolar malignant syndrome. EPS effects
seen less and autonomic
disorder. (anticholinergic and alpha block)
are more in low potency drug
EPS are less common so they are

more prefereble, Clozapine can
Alleviate the positive and cause agranulocytosis, metabolic
negative symptoms both.
effects like weight gain,
hyperglycemia.
Name of Route of administration Receptor affinity and
agent action
Morphine Oral and parenteral mu agonist-strong (full)
Methadone Oral and parenteral mu agonist-strong (full)

Meperidine Oral and parenteral mu agonist-strong (full)
Buprenorphine Parenteral mu agonist-partial
Codeine Oral and parenteral mu agonist-partial (weak)
Propoxyphene Oral mu agonist-very weak
kappa agonist weak mu
Nalbuphine Parenteral antagonist
kappa agonist weak mu
Pentazocine Parenteral
antagonist
Parenteral, sublingual, mu antagonist-strong
Naloxone
intralingual, submental & nasal. (competitive)
Naltrexone Parenteral oral mu receptor antagonist

(competitive)
Butorphanol Parenteral kappa receptor agonist and mu

receptor partial agonist
weak kappa, delta and mu

Tramodol Oral
receptor agonist
Therapeutic effects Other
Strong analgesia Marked sedation, poor oral bioavailability, histamine release
Strong analgesia Oral activity and long duration.

Strong analgesia M blocker, forms normeperidine, seizures.
Analgesia Long action because binds tightly to receptor
Weak Analgesia Weak analgesia but additive with acetaminophene or ASA
Weak Analgesia Toxic in OD and difficult withdrawal
Analgesia, sedation Less abuse liability than other storng opioids
Fair Analgesia, sedation May impede effects of mu agonist
Treatment of opioid OD and Decreases craving in alcoholism also used as antidote in opioid
alcohol opioid dependence poisoning
Treatment of opioid OD and Decreases craving in alcoholism
alcohol opioid dependence
Analgesia, sedation Has the lower risk of respiratory depression
Inhibits serotonin and noradrenaline reuptake, can increase a

Analgesia, sedation
risk of serotonin syndrome, Strong addictive potential
Organ system Receptor Sympathomimetic effect
α1 Mydriasis (↑ pupillary dilator muscle contraction)
Eye α2 ↓ Aqueous humor production
β2 ↑ Aqueous humor production
Venoconstriction → ↑ venous return → ↑ preload
α1 ↑ Vascular smooth muscle contraction of arterioles → ↑
peripheral resistance → ↑ afterload
Blood vessels
α2 ↑ Platelet aggregation
Peripheral vasodilation → ↓ peripheral resistance →
β2 ↓ afterload
↑ Heart rate
Heart β1 ↑ Contractility
↑ Automaticity and conduction velocity
Bronchi β2 Bronchodilation
α1 Sphincter contraction
Gastrointestinal tract
β2 ↓ Peristalsis
α1 ↑ Glycogenolysis
Liver
β2 ↑Gluconeogenesis (β2 activation)
α2 ↓ Insulin release
Pancreas
β2 ↑ Insulin release
Kidneys α1 ↓ Release of renin
β1 ↑ Release of renin
α1 Sphincter contraction → urinary retention
Bladder
β2, β3 Detrusor muscle relaxation
Female repro. organs β2 ↓ Uterine tone (tocolysis)
Male repro. organs α1 Ejaculation from vas deferens
↑ Contraction
β2
Skeletal muscle ↑ Glycogenolysis
β3 ↑ Thermogenesis in skeletal muscle
α2 ↓ Lipolysis
Adipose tissue
β1–3 ↑ Lipolysis
Target organs Receptors Parasympathetic nervous system
Brain M1 CNS (increase memory, attention)
Miosis
Eye M3
Focus on near objects (accommodation)
Salivary glands M3 ↑ serous secretion
Vasodilation: - e.g., deep arteries of
Blood vessels M3 the penis (cavernosal arteries) during erection. Indirectly: via
withdrawal of tonic adrenergic vasoconstriction. Most blood
vessels in the body do not have parasympathetic innervation.
↓ Heart rate (negative chronotropic)
Heart M2
↓ Contractility (negative inotropic)
↓ Conduction velocity (negative dromotropic)
Lungs M3 Bronchoconstriction
M1 ↑ gastric acid release
Stomach, intestine
M3 Sphincter dilation, ↑ motility
Pancreas M3 ↑ insulin secretion, ↑ exocrine secretion
Liver: M3 ↑ gluconeogenesis
Reproductive organs M2 ♂+♀ erection
Bladder M3 Relaxation of vesical sphincter muscle, Contraction of detrusor

muscle
Agents MOA
Direct acting cholinomimetic- M

Bethanechol selective resistant to AChE
Methacholine Direct acting cholinomimetic- M>N

causes hydrolysis of AChE+
Pilocarpine Direct acting cholinomimetic- M

selective resistant to AChE
Direct acting cholinomimetic- M

Carbachol
selective resistant to AChE
Indirect acting cholinomimetic-

Physostigmine reversible AChE inhibitor, also
stimulates M and N receptors.
Duration 2-4 hrs

Neostigmine reversible AChE inhibitor. Duration
2-4 hrs

Pyridostigmine reversible AChE inhibitor. Duration
3-6 hrs
Edorphonium reversible AChE inhibitor. Duration
10-20 mins
Isoflurophate (DFP) irreversible AChE inhibitor.
Organophosphate ages in 6-8 hrs
1. Echothiophate Indirect acting cholinomimetic- long
2. Malathion, parathion acting irreversible AChE inhibitor.
3. Sarin Organophosphates.
Muscuranic Antagonist.
Atropine
CNS entry.
Scopolamine Reversible.
Ipratropium No CNS entry
Tropicamide
CNS entry
Glycopyrrolate
CNS entry
Benztropine, Muscuranic Antagonist.
Trihexiphenidyl CNS entry
Hexomethonium Ganglionic blocker
Mecamylamine Ganglionic blocker
Postoperative illeus, urinary retention also Salivation, sweating, flushing, decrease BP,
postoperative and postpartum nausea, abdominal pain, diarrhea and
nonobstructive urinary retention. bronchospasm.
Diagnosis of bronchial hypersensitivity -
Treatment of glaucoma as it opens the

trabecular network around schlemm -
(topical) and induces sweat, tears and saliva
(tx of xerostomia)
Treatment of glaucoma as it increases flow

through canal of schlemm, cause miosis and -
decrease intraocular pressure.
Antidote for overdose of atropine,

phenothiazines and TCAs,Tx of glaucoma Convulsions at high doses, bradycardia and
cause miosis and decrease intraocular skeletal muscle paralysis seen with
pressure, intestinal and bladder atony is therapeutic doses.
treated.
Tx of postoperative illeus and urinary

Salivation, sweating, flushing, decrease BP,
retention and myasthenia gravis, reversale nausea, abdominal pain, diarrhea and
of neuromuscular blockers (tubocurarine,
etc.). bronchospasm.
Chronic management of myasthenia gravis. -
Dx of myasthenia gravis and IV injection -

lead to an increase in muscle strength
Generalized cholinergic symptoms, paralysis

Chronic tx of open angle glaucoma. of motor function (difficulty breathing,
convulsions, miosis.
1. Rx glaucoma
2. Used as insecticides -
3. Used as nerve gas
Dry mouth, blurred vision, ‘sandy eyes’,

Antispasmodic, Antisecretory, Management tachycardia and constipation. CNS include
of AChE inhibitor overdose, Antidiarrheal, restlessness, confusion, hallucinations, and
Opthalmology (long action so not ideal) delirium progress to depression, collapse of
respiratory and circulatory system
More effect on CNS than atropine, used in
antimotion sickness, sedative high doses
may cause excitement. Short term memory -
block so used as anesthetic procedures
Used in asthama and in COPD management. -
Othalmological use topical. -
Antispasmodic, antisecretory and antiulcer -
Used in parkinson and drug induced -

extrapyramidal symptoms.
NO use it is just a prototype only reverse -
the reflex bradycardia or tachycardia -
Muscuranic effects are DUMBBELSS- Diarrhea,
Urination, Miosis, Bradycardia, Bronchospasm,
Emesis, Lacrimation, Salivation, Sweating.
Agents MOA
Direct acting sympathomimetics,

Epinephrine
α1, 2, β1 and 2 agonist

Norepinephrine α1, 2 and β1 agonist.
α1> α2> β1
Dopamine Direct acting sympathomimetics

(Fenoldopam) D1= D2 > β1 > α1

Isoproterenol β1 = β2

Dobutamine β1 > β2, α (initially was believed β1
selective agonist).
Phenylephrine Direct acting agonist

α1 agonist
Direct acting agonist

Midodrine α1 agonist
Methoxamine
α1 agonist
Oxymetazoline Direct acting agonist

α1 agonist

Clonidine
α2 agonist

Methyldopa
α2 agonist
Dexmedetomidine α2 agonist
Salmeterol, Albuterol,
Metaproterenol, Direct acting agonist
β2 agonist
Terbutaline, Ritodrine
Methylphenidate Indirect acting agonist

Amphetamine like
Indirect acting agonist
Tyramine Amphetamine like
Cocaine Indirect acting agonist

Amphetamine like
Mixed acting or indirect acting
Ephedrine
sympathomimetic
DOC for type 1 hypersensitivity reactions, anaphylatic

shock, Bronchospasm, glaucoma (vasoconstriction of Anxiety, fear, tension, headaches, tremor,
bld vssles of ciliary body and lessen the aqueous cerebral hemorrhage due to elevated BP,
humor, adjunct to local anesthetics (increase cardiac arrhythmias, pulmonary edema
duration)
Hypertension and reflex bradycardia,
Used to treat shock as it causes increase PVR and BP Piloerection, Urinary retention, Ischemia and
necrosis or fingers toes epsecially.
DOC for hypovolemic and cardiogenic shock as at high

doses causes vasoconstriction, beta 1 and 2
stimulation positve inotropic and chronotropic effects Nausea, hypertension, arrhythmias.
and at low dose renal vasodilation at low doses
increase renal bld flow.
Positive inotropic and chronotropic effects, dilation of

skeletal muscle arteries, Used in asthma Similar to epinephrine.
(bronchodilation)
Positive inotropic and chronotropic effects, dilation of

skeletal muscle arteries, used for acute congestive Tolerance with prolonged use, tachyphylaxis.
heart failure.
Effective in mydriasis without cycloplegia, Hypertension and reflex bradycardia,

Piloerection, Urinary retention, Ischemia and
decongestant (rhinitis), can be used to increase BP necrosis or fingers toes epsecially.
Tx of orthostatic hypotension, due to ANS

impairement -II-
Used in paroxysmal atrial tachycardia (vagal reflex =

-II-
bradycardia), or hypotensive states.
Rhinitis, epistaxis, sinusitis
Used in sympatholytic effect in treating HTN, diminish Abrupt Discontinuation can lead to rebound
craving of narcotic and alcohol withdrawal can
facillitate smoking cessation. HTN.
Anti-hypertensive drug especially in pregnancy. -
Indicated for sedation in intubated and mechanically

intubated patients. -
Used in asthma, Reduce premature labor. -
Used in children with ADHD -
In patient treated with MAO inhibitors marked

increase in BP -
Local anesthesia, vasoconstriction -
Used for anesthesia induced hypotension, urinary

-
incontinence, nasal descongestant.
Agents MOA
Propanolol Non selective, Competitive β

antagonist.
Metoprolol, Atenolol, Esmolol,

Bisoprolol,
Betaxolol, Bevantolol, Selective β-1 antagonist.
Nebivolol, Acebutolol,
Celiprolol
Pindolol, Penbutolol, Oxprenolol,

Propranolol, Nadolol, Sotalol, Non selective β-1, 2 and 3
Timolol, Tertalol, Labetalol, antagonist. Also α1 antagonist.
Bucindolol, Carvedilol
Non selective α receptor

Phentolamine reversible competitive
antagonists. Short duration.
Non selective α1 and 2 receptor

Phenoxybenzamine irreversible antagonists. Long
duration.
Prazosin, Doxazocin, Terazosin α1 selective compitetive

antagonist
Tamsulosin, alfuzosin, silodosin α1 selective compitetive

antagonist
Yohimbine α2 selective antagonist

Used in HTN, Glaucoma, Hyperthyroidism, Bronchoconstriction, arrhythmias (drug
migraine, angina pectoris, post MI, never be stopped quickely), male sexual
performance anxiety. impairment, fasting hypoglycemia
Used with great caution in asthma, safe in Bradycardia, Bradyarrhythmia,

diabetes, bronchoconstriction, Coronary Cardioselectivity is dose-
heart disease, Compensated heart failure,
Acute coronary syndrome, Cardiac dependent: β2 receptor blocking activity
increases with higher doses.
arrhythmias.
Topical opthalmic application in glaucoma -
Agonist effect at muscuranic and H1 and 2

receptors, used for diagnosis and Tx for Severe tachycardia, arrhythmias and
pheochromocytoma and in orthostatic myocardial ischemia
hypotension
Reduces BP when sympathetic tone is high. Orthostatic hypotension and tachycardia;

DOC for pheochromocytoma Inhibition of ejaculation; Nasal stuffiness;
Less specific CNS effects à fatigue, sedation
and nausea
Used for mild to moderate HTN and inhibits
prostatic smooth muscles so used in BPH Orthostatic hypotension and retrograde
Lowers the PVR and BP, lessens the reflex ejaculation.
tachycardia.
Inhibits prostatic smooth muscles so used in Orthostatic hypotension and retrograde
BPH ejaculation.
Used in orthostaic hypotension and in
impotence or erectile dysfunction. -
Pheochromocytoma (High
blood pressure,
Headache,Heavy sweating,
Rapid heartbeat)
Agents MOA
Terbutaline, Albuterol Short acting selective β2 agonists

Metaproterenol, Pirbuterol Oral administration
Long acting selective β2 agonists

Salmetrol, Formeterol
Oral administration
Theophylline Inhibit the enzyme PDE4 → ↑cAMP and

inhibit adenosine
Ipratropium M3 Antagonists
Tiotoprium Inhaled preparation
Beclomethasone, budesonide Corticosteriods

(Pulmicort), ciclesonide*,
Phospholipase A2 inhibitor, inhibit
flunisolide, fluticasone (Flovent), transcription factors (e.g., NF-κB) → ↓
mometasone, triamcinolone,
dexamethasone. expression of pro-inflammatory genes
Zileuton Selective inhibitor of 5-lipoxygenase
Zafirlukast, Montelukast LTD4 receptor antagonist
Cromolym, Nedocromil Prevent degranulation from mast cells

Actions and indication Side effects
Bronchodilation within 15-30 mins and persist for Skeletal muscle tremor, nervousness,
3-4 hrs. Used for short term treatment of asthma. occassional weakness.
Actions is long acting for 12hrs, used along with

glucocorticoids for moderate and severe
-
persistent chronic asthma, also helpful in exercise
induced asthma.
Short term relief of asthma. CNS excitation, diarrhea, nausea, arrhythmias,

positive iono and chronotropic effects
Short term relief of asthma. Valuable for patients
using beta blockers. First line treatment for COPD
(Tiotrprium)
Oral and parenteral administration. Used in long

Osteoporosis, cataracts, slow growth rate in
term treatment of asthma also for the patients childrens
that require urgent treatment.
Adjunctive therapy along with steriods Asthenia, headache, liver toxicity (pts should be
monitored for signs of hepatitis)
Used prophylactically for forms of asthma, Adverse effects: (minimal) diarrhea, headache,
including antigen, exercise or drug induced increased infections
Only value when taken prophylactically. Throat irritation, cough and mouth dryness.
Type Agent MOA
Sodium Bicarbonate (NaHCO3) Weak Bases acting with Gastric HCL and form
Calcium Bicarbonate (CaCO3) salt and water.
Antacids
Aluminium Hydroxide Al(OH)3 Reacts slowly with acid and form
Magnesium Hydroxide Mg(OH)2 aluminium/magnesium chloride and water
H2 receptor Cimetidine, Ranitidine

Blocks histamine 2 receptors
antagonists Famotidine, Nizatidine
Intermittent heart burn and dyspepsia Metabollic alkalosis and bleching
Intermittent heart burn and dyspepsia, pt

Al(OH)3 Constipation, Mg(OH)2 Diarrhea
with renal insufficiency should be careful
Gastritis, peptic ulcer disease, GERD and Diarrhea, headache, fatigue, myalgias,
acute stress ulcer. constipation, confusion, hallucinations.
Types Agents
Standard penicillin Penicillin G & V
Antistaphalococcal Methicillin, nafcillin, oxacillins.

penicillins
Aminopenicillins Ampicillin, amoxicillin
Carboxypencillis (carbecillin,
Antipsuedomonal ticarcillin), Ureidopenicillins
penicillins (piperacillin, azlocillin,
mezlocillin)
Clavulanic acid, Avibactam,

Beta lactamase inhibitors
Sulbactam, Tazobactam.
Cephalexine, Cefazolin,
Cephalosporins 1st gen. Cephradine, Cefadroxil.
Cefuroxime, Cefoxitin,
2nd gen. Cefamandole, Cefotetan,
Cefaclor
Cefotaxime, Ceftriaxone,
3rd gen. Ceftazidime, Cefoperazone,
Cefixime.
4th gen. Cefepime, Cefpirome
5th gen. Ceftaroline, Ceftobiprole
Carbapenems Imipenem, Meropenem,

Ertapenem, Doripenem
Monobactam Aztreonam
Vancomycin
Fosfomycin
Others
Bacitracin
Cycloserine
MOA Actions and indication
Bind to PBP, inhibit crosslinking of
peptide chain of bacterial cell wall, Pen.G DOC for N.meningitidis, T.pallidum, C.difficle,
perfringes, Dipthteriae, Actinomyces.
Penicillase sensitive, BACTERICIDAL

peptide chain of bacterial cell wall, Used only against Penicillinase producing
staphylococci.
Penicillase resistant, BACTERICIDAL
Bind to PBP, inhibit crosslinking of Ampicillin is DOC for listeria, also against E. coli, H.
peptide chain of bacterial cell wall, influenza, Listeria monocytogenes, Salmonella and
Penicillase sensitive, BACTERICIDAL Shigella.

peptide chain of bacterial cell wall, Against pseudomonas and enterococci
Penicillase sensitive, BACTERICIDAL
Inhibits Beta lactamases enzymes Used in combination with lactamase sensitive agents

peptide chain of bacterial cell wall, Cefazolin DOC for surgical prophylaxis
-II- H.influenza, N.menigitidis, moraxxella catarrhalis.

Activity against anaerobes (cefotetan).
Gram +ve and -ve cocci, and gram -ve rods, resistant
-II-
to lactamases.
-II- Cefepime combined with ceftazidime against

psuedomonas.
Ceftobiprole anti psuedomonal, ceftaroline is for
-II- community accquired pneumonia and infections.
peptide chain of bacterial cell wall, DOC for infections due to enterobacter.
Monobactam inhibitor of early step in Resistance to beta lactamases, against gram -ve rods,
cell-wall synthesis, binds to peniciilin hospital acquired pneumonia (mainly)
binding protein 3 Penicillase resistant
Bind at D-ala D-ala pentapetite hinder
transglycosylation and interferes cross MRSA DOC, gram +ve cocci, enterococci, anaerobes,
linking, Penicillinase and methicillin C. difficle, against pneumococci resistant to penicillin.
resistant.
Agent blocks the inhibition of enzyme Against both gram +ve and -ve, safe in pregnancies.
endopyruvate transferase
Mixture of polypeptides that inhibit

Active against gram +ve
bacterial cell wall synthesis.
Against gram (+) and gram (-) organisms, but is used

Inhibit enzymes D- alanine ligase and almost exclusively to treat tuberculosis caused by
alanine racemase. strains of Mycobacterium tuberculosis resistant to
first-line agents
Side effects
Hypersensitivity, neurotoxicity, Platelet

dysfunction (Carbenicillin, Ticarcillin), GI
distress, Nephrotoxicity (Methicillin),
Neutropenia (Nafcillin), Cation toxicity:
sodium / potassium
Pain at site, thrombophebititis,

hypersensitivity reactions, cross
hypersensitivity with penicillins, renal
toxicity, bleeding (hypothrombinemia),
disulfiram like reaction.
GI distress, cross allergies with penicillins,

seizures and renal dysfunction (imipenem)
-
Phlebitis in the site of action, red man
syndrome, nephrotoxicity, ototoxicity.
Restricted to topical application for

treatment of minor skin and ocular infections,
because of its potential for nephrotoxicity
Serious dose-related CNS toxicity

Headaches, tremors, acute psychosis,
convulsions
Types Agents MOA
Binds to receptors 30s unit of

Streptomycin, gentamicin, ribosome, inhibit the initiation
complex formation and cause
paromomycin, neomycin, misreading of mRNA in non toxic
Aminoglycosides kanamycin, amikacin
BACTERICIDAL also enters bacteria via O2
reuptake
Spectinomycin Structurally related to

aminoglycosde
Binds to receptors 30s unit of

Tetracyclines Doxycycline, minocycline, ribosome, inhibit the initiation
BACTERIOSTATIC demeclocycline complex formation and prevents
the addition of new amino acids.
Macrolides
BACTERIOSTATIC Erythromycin, Azithromycin, Irreversible bind to 50s unit and
clarithromycin, Dirithromycin, inhibit the translocation step.
BACTERICIDAL at
high doses Spiramycin. Eryth, clar inhibit cyp450
BACTERIOSTATIC Chloramphenicol Binds to 50s unit and inhibit

peptidly transferase enzyme.
Not a macrolide but mechanism

BACTERIOSTATIC Clindamycin same as macrolide
Blocks 70s ribosome assembly by

BACTERIOSTATIC Linezoid
binding to 50s subunit.
Binds to separate site on 50S

BACTERICIDAL Quinipristine/ Daflopristine ribosome and interrupt protein
synthesis
Streptomycin DOC for bubonic plague and

tularemia. Other uses are gram (-) septicemia, Nephrotoxicity, Ototoxicity,
urinary tract infections, pneumonia,
peritonitis, infections of skin and mucous neuromuscular blockade, contact
dermatitis
membranes, preparation of bowel for surgery,
adjunct therapy in hepatic coma
Used in alternative treatment of gonorrhea -
First choice drug for chlamydia infections, GI distress, tooth enamel dysplasia and
rickettsia, mycoplasma pneumonia, borrelia dcreased bone growth (binds to Ca, Mg,
burgdorferi. Also used in brucelliosis, plague, Fe) hepatotoxicity, phototoxicity, renal
tularemia, cholera, granuloma inguainal and in dysfunction (except Doxycycline),
ACNE. pseudotumor cerebri.
corynebacterium, chlamydia, syphillis, GI distress, drug interaction, reversible

mycoplasma, bordetella, legionellosis (DOC
deafness at high doses or (clarithr.)
azithromycin), sinusitis, otitis media.
Dose dependent bone marrow

Bacteroides including B. fragilis, H. influenzae, supression, gray baby syndrome, optic
N. meningitidis, rickettsiae, salmonella typhi neurititis.
Narrow spectrum: gram (+) cocci and

Rash, psuedomembranous colitis,
anaerobes including B. fragilis (backup drug), impaired liver function neutropenia.
has also been used in toxoplasmosis
Vancomycin resistant Staph Aureus (VRSA), Inhibit MAO, GI distress,

vancomycin resistant enterococci (VRE) throbocytopenia, serotonin syndrome.
Vancomycin resistant Staph Aureus (VRSA), Venous irritation, hyperbilirubinemia,

vancomycin resistant enterococci (VRE) arthralgia, ihibit cyp450
Resistance
Bacterial conjucated enzymes,

mutation of proin protien of O2,
mutation of receptor of 30s.
Bacterial conjucated enzymes,

efflux pump, decreased uptake.
Resistance in gram (+) bacteria

involves production of a
methylase that adds a methyl
group to the ribosomal binding
site
Resistance has been reported

via formation of inactivating
enzymes and increased efflux
mechanisms
Agents MOA
Sulfisoxazole,
sulfadiazine,
sulfamethoxazole, Competes with PABA and Inhibits
sulfadoxine,
Sulfacetamide, enzymes:- Dihydropteroate
Sulfasalazine, synthatase (sulfonamides),
Dihydrofolate reductase
Mafenide, Silver (Pyrimethamine, Trimethoprim)
sulfadiazine,
Pyrimethamine,
Trimethoprim.
Single Use:- DOC for nocardia

(Cotrimazole)
Simple UTIs (sulfiox, sulfamethaxole),
trachoma (sulfacetamide), burn dressing
and ulcers (silver sulfadiazine)
Combination Use:- DOC tripmethoprim Cystalluria, steven johnson, GI distress,
and sulfamethoxazole in pneumocyctis in phototoxicity, dermatitis, hemolysis in
HIV pts. G6DP deficiency in dose dependent
Sulfadoxine with pyrimethamine in manner, kernicterus in new born.
resistant malaria, Sulfadiazine with
pyrimethamine in toxoplasmosis,
Sulfasalazine (5-ASA) with sulfapyridine
for ulcerative collitis and rheumatoid
arthritis.
Resistance
Increased formation of PABA,

structural changes in synthetase,
decreased intracellular
accumulation, utilization of folate
from exogenous sources
Agents MOA
Norfloxacin, Ciprofloxacin,
Ofloxacin, Pefloxacin, Block DNA synthesis by inhibiting
Levofloxacin, Sparfloxacin, enzymes Topoisomerase II (DNA
Gatifloxacin, Moxifloxacin, gyrase), Topoisomerase IV
Trovafloxacin
Typhoid fever (S. typhi) GI distress, Rash, Phototoxicity

(Sparfloxacin), Insomnia, dizziness,
(Ciprofloxacin(DOC), Levofloxacin), headache, Seizures occur in OD and in
Gonorrhea (Ciprofloxacin and Ofloxacin),
Community acquired pneumonia susceptible pts. Tendonitis and
Spontaneous tendon ruptures
(Levofloxacin), Anthrax (Ciprofloxacin is
DOC), Gastroenteritis, UTI, Meningitis, (Ciprofloxacin), QT prolonged
(Sparfloxacin), Hepatotoxicity
Urogenital and soft tissue infections (Trovafloxacin)
Resistance
Increasing via increased drug

efflux (P. aeruginosa), Via
changed sensitivity of target
enzymes: Topoisomerase IV :
gram (+) cocci (Staph)
Topoisomerase II : (E. coli)
Agents MOA
Prodrug converted to activated form by

Isoniazid enzyme catalase perioxidase by Kat G gene
BACTERICIDAL of mycobacteria resulting in inhibition of
cell wall synthesis and is slow acetylator.
Rifampin (inducer of
cyo450), rifapentin, Inhibits DNA dependent RNA polymerase
enzyme by binding to beta subunit which
rifabutin, rifampicin blocks the transcription and RNA synthesis
BACTERICIDAL
Pyrazinamide Inhibit the growth of M.tuberculosis by

BACTERICIDAL decreasing the ambient pH
Ethambutol Inhibit sythesis of arabinogalactan (cell wall

BACTERIOSTATIC component)
Active against M.tuberculosis. Drug Hepatitis, peripheral neuritis (pyridoxine

interaction inhibits metabolism of deficency), toxic encephalopathy, seizures,
phenytoin increasing its toxicity anemia, thrombocytopenia.
Hepatitis, hypersensitivity flu like,

Alternative of INH in tuberculosis in HIV thrombocytopenia, Red orange metabolities
patients, N.meningitidis for close contacts
and H.influenza, Staph.aureus (rifampicin) in urine, tears and other body fluids.
Uveitiitis, dyspepsia
Hepatitis, hyperuricemia (gout), polyarthalgia,

Administered along with INH and Rifampin
for first 2 months of treatment myalgia, rash, phototoxicity, increased
porphyrin synthesis
Combined with other drugs (INH,

Rifampin, Pyrazinemide) to prevent Retrobulbar neuritis, hepatitis,
development of resistance in case thrombocytopenia.
resistance is suspected
Resistance
Mutation of Kat G gene,

overexpression of InhA.
Decreased affinity to RNA

polymerase
-
Agents MOA
Polyenes
Amphotericin B, Interacts with ergosterol and form pores
Nystatin FUNGICIDAL
Enter inside via viral cytosine permease and

then get converted to its active form by viral
Flucytosine enzyme cytosine deaminase 5- FU that inhibits
enyzme thymidylate synthetase that alter DNA
synthesis. FUNGISTATIC
Interferes with ergosterol synthesis by

Ketoconazole inhibiting the enzyme 14-α-demethylase.
Inhibit cyp450, proton pump & H2 blocker
Azoles -II- excellent CNS permeablity

Fluconazole FUNGICIDAL (all azoles)
Itraconazole -II- poor CNS permeability
Capsofungin, Inhibit synthesis of Beta(1-3)-D-glucan. Only IV

Echinocandins mucafungin,
available.
anidulafungin.
Interact with microtubules and inhibits
Griseofulvin mitosis. Inducer cyp450, 3A4
FUNGISTATIC.
Terbinafine Inhibits the enzyme squalene epoxidase

Actions and indication
DOC (or co-DOC) for severe infections caused by
Aspergillus, Cryptococcus & candida (synergist with
flucytosine), Histoplasma, Mucor, Coccidioides, no CNS
penetration but can be used intrathecally.
Used in combination with amphoterecin B for candiasis

and cryptococcos infection. Enters CSF
Co-DOC for Paracoccidioides and backup for

Blastomyces and Histoplasma, absorption impared by
antacids (oral and topical).
Azole of choice for prophylaxis and supression in
cryptococcal meningitis, single dose can eradicate
vaginal candiadis.
DOC for Blastomycosis and Sporotrichoses, good
against dermatophytes (onychomycosis)
Against Candida and aspergillus
Only against dermatophytes (drug concentrate in areas

with keratin)tx mainly of tinea capitus. Contraindicated
in pts porphyria
Against dermatophytes and candiasis and superior in
onychomycosis that grisefulvin
Side effects Resistance
Infusion related IV infusion hypertension and
dose related nephrotoxicity. Abnormalities of Fungal strains appear to
have low ergosterol,
liver function tests, Anemia, leukopenia, modify sterol target.
thrombocytopenia, Cardiac arrythmias
Hematotoxicity (BM supression), GI distress, Rapidly by reducing

hepatic dysfunction. enzymes.
GI detress, decre. Libido, gynecomastia,

amenorrhea (block androgen and steriod syn.),
dilsulfiram like.
Via decreased
accumulation of azoles
N/V, Hepatotoxicity, Hypokalemia, Hypotension,
Edema, Headache
Allergic reactions, phototoxicity, nausea and

headaches, hepatotoxicity, teratogenic
GI distress, headache, taste and visual

disturbances, hepatic dysfunction, rash
Agents MOA
Acyclovir (Guanine
analog) All drugs are phosphorylated by a
viral thymidine-kinase, then
converted to nucleotide analogs
Gancyclovir (Guanine (triphosphorylated form) by host
analog) cell kinases
Phosphorylated form inhibits
Cidofovir (cytosine viral DNA-polymerase
analog)
Foscarnet (inorganic Directly inhibits DNA and RNA

pyrophosphate
analog) polymerase
Antisense oligonucleotide against

Fomiversin
CMV
Converted by cellular enzymes to
Vidarabine triphosphate analog which
inhibits DNA polymerase
Converted by cellular enzymes to
Trifluridine triphosphate analog which
inhibits DNA polymerase
Amantidine, Inhibit viral uncoating
rimantidine
Oseltamivir, Neuraminidase inhibitors
Zanamivir (prevent realease of virons)
Ribavarin Inhibit RNA polymerase
Lamivudine, adefovir, Inhibit replication of HBV

Entecavir.
Actions and indication
DOC Genital HSV infections, Reduces viral shedding,
Herpes labialis (cold sore), HSV encephalitis , HSV
infections in immunocompromised patient
DOC CMV retinitis in immunocompromised patient,
Prevention of CMV disease in transplant patients, CMV
infections in AIDS
CMV retinitis in immunocompromised patient.
Against acyclovir and gancyclovir resistant strains
CMV strains resistant to Ganciclovir, Cidofovir, and

Foscarnet
HSV keratoconjunctivitis (topical) in

immunocompromised patient.
HSV keratoconjunctivitis and acyclovir HSV resistant

strain. HSV 1, 2 and VZV
Prevention and treatment of infulenza A
Effective against both type influenza A and B
Only effective against RNA viruses (DOC for Respiratory

syncycial virus and lassa virus. Alternative for hep C (with
IFN α2b), measles, mumps, etc.)
Lamivudine HIV and HBV hepatic viral infections

Entecavir lamivudine resistant HBV
Side effects Resistance
Cystalluria, neurotoxicity (seizures in OD).

Changes in DNA
polymerase, Decreased
Hematotoxicity, mucositis, fever, rash, cystalluria, activity of thymidine
seizures in OD kinase
Nephrotoxicity.
Nephrotoxic, neurotoxic, hypocalcemia and

hypomagnesemia.
Iritis, vitritis
Neurotoxicity, headache, tremor, confusion, seizures,

Anemia, leucopenia, thrombocytopenia, SIADH
Amantidine antiparkinsonin effects livedo reticularis
Risk of bronchospasm with zanamivir
Anemia, jaundice and teratogenic
-
Type Subtype Agents
Methotreaxate
Folate Antagonist
Pemetrexed
5-Flurouracil
(Capecitabine produrg)
Pyrimidine Antagonist
Cytarabine
DNA Synthesis 6-Mercaptopurine

Inhibitors Azathioprine
Purine Antagonist
Thioguanine
Fludarabine
Purine Analogs
Cladribine
Ribonucleotide reductase Hydroxyurea

inhibitors
Vinblastin
Vinca Allkaloids
Mitotic Inhibitors Vincristin
Paclitaxel
Taxanes
Docetaxel
Camptothecan analogs:-
Topoisomerase I inhibitor Irinotecan
Topoisomerase Topotecan
inhibitors Podophyllotoxins:-
Topoisomerase II
Etoposide
inhibitor Teniposide
Cyclophosphamides
Nitrogen mustards
Ifosfamide
DNA Alkylating Carmustin
agents Nitrosourea drugs
Lomustin (cross BBB)
DNA Alkylating
agents
Platinum compounds Cisplatin, carboplatin,

orboplatin
Others Busulfan
Duanorubicin
Anthracycline drugs
Doxorubicin
DNA Intercalating
agents
Bleomycin (moa same as
Others metranidazole)
MOA Indications
Inhibit enzyme dihydrofolate reductase Breast cancer, nonHL, osteosarcoma, ALL

Leucovorin is used with methotrexate as
rescue drug. Medical abortion, ectopic pregnancy,
immunosupression
Inhibit enzyme thymidylate synthetase Urothelial cell carcinoma, topical for keratosis
and non invasive skin tumors
Inhibit DNA polymerase i.e inhibit DNA

Combined with daunorubicin to treat AML
elongation
Bioactivated by HGPRT (6-M…), form ALL, AML, SLE. 6-Mercaptopurine is metabolized

by xanthine oxidase (Allupurinol doses should be
purine analogs and decrease DNA reduced otherwise active metabolites of 6-MP
replication.
will increase and cause toxicity).
CML, non-HL
Insert triphosphate metabolites causing
DNA chain termination. Cladribine inhibit
adenosine deaminase Hairy cell leukemia.
Inhibits enzyme ribonucleotide reductase CML, ovarian cancer and melanoma

cells accumulate in S phase
ALL, HL, non-HL, multiple myeloma,
Bind to tubulin and blocks its neuroblastoma.
polymerization
Bladder, breast, ovarian, testicular, cancers
Bind to tubulin and blocks its Metasatic breast and ovarian cancer, non small
depolymerization cell lung cancer. Act in M phase.
Irinotecan: colorectal cancer, Topotecan: lung,

Inhibit breaking and resealing of ssDNA ovarian cancer, glioma, sarcoma.
Inhibit breaking and resealing of dsDNA AML, ALL, testicular, lung cancer and non-HL
ALL, CLL, non-HL, neuroblastoma, ovarian

cancer.
Alkylation of DNA/RNA → cross-links

DNA at guanine N-7 → impaired DNA Excellent CNS penetration used to treat brain
synthesis tumors (astrocytomas)
Alkylation of DNA/RNA → cross-links
DNA at guanine N-7 → impaired DNA
synthesis
Testicular, ovarian, bladder, cervical and lung

cancer.
CML.
AML
Intercalation of DNA, inhibition of HL, breast, bladder, ovarian cancer
topoisomerase, formation of free
radicals, Bleomycin more effective on
neoplastic cells in G2 phase. HL, non-HL, testicular, head, neck cancer
Adverse effects
BMS, long term use hepatotoxicity
mucocutaneous ulcers stomatitis
BMS, GI irritation, alopecia, plantar-

palmar erythrodysesthesia
BMS, oral and GI ulceration,

pancytopenia (Cytrabine)
Hepatotoxicity, GI distress
BMS, nephro and neurotoxicity
Rapid onset of BMS
BMS, alopecia
Neurotoxicity (peripheral neuropathy)
BMS, alopecia, neuropenia,

neurotoxicity.
BMS, alopecia, diarrhea
BMS, alopecia
Produces toxic acrolein which causes

hemorrhagic cystitis can be treated with
mercaptoethanesulfonate (mesna)
which binds to acrolein, hepato and
cardiotoxicity, SIADH
Prolonged BMS, pulmonary damge

Neurotoxicity (ototoxicity),
nephrotoxicity (use amifostin) and
highly emetogenic (use odansetron)
Pulmonary fibrosis, hepatotoxicity
Free radicals cause congestive heart
failure (use dexrazoxane)
Pneumocistis that progress to
pulmonary fibrosis, mucocutaneous
reactions.
Type Agent
Imatinib
Erlotinib
Protein Kinase Inhibitors
(all of them inhibit tyrosine Sunitinib, Sorafenib
kinase which is an
oncoprotein)
Gefitinib
Lapatinib
Cyclosporine
Tacrolimus
Immunosuppressant
agents
Sacrolimus (Rapamycin)
Mycophenolate Mofetil
Immunosuppressant and
Thalidomide
stimulant both
Abciximab
Daclixumab
Infliximab
Muromonab (OKT3)
Monoclonal Antibodies
Palivizumab
Natalizumab
Rituximab
Trastuzumab
MOA Indication
Inhibits c-kit i.e a BCR ABL tyrosine kinase stem cell First line treatment for CML. Used to treat GI stromal
receptor. tumors
Highly specific tyrosine kinase inhibitor associated with Second line treatment for non small cell lung and
epidermal growth factor. pancreatic cancer.
Inhibit multiple receptor tyrosine kinase including For advanced renal cell carcinoma.
VEGFR and c-kit.
Targets epidermal growth factor receptors For non small cell lung cancer.
Inhibit kinase associated with HER-2 receptors For breast cancer
Inhibit calcinuerin by binding to cyclophyllin that result Used to prevent rejection of organ transplants usually
in inhibition of production and relase of IL-2 given with combination of cortitosteriods. Also
Inhibit calcinuerin by binding to FK-506 protien that cyclosporines can be used for rheumatoid arthritis ,
result in inhibition of production and relase of IL-2 asthma, uveitis, DM type I, psoriasis.
Inhibits mTOR involved in T-cell proliferation, i.e inhibits

the response of T cells to cytokines without affecting Used to prevent rejection of organ transplants.
cytokine production.
Inhibition of inosine monophosphate dehydrogenase Used in combination with cyclosporin or tacrolimus as

leads to selective inhibition of lymphocyte proliferation transplant rejection prophylaxis
Used to tx cancer, recurrent aphthous ulcers, Tb,

Inhibit IL-2, TNF-alpha and may stimulate CD8 leproxy, erythema nodosum leprosum and the AIDS-
associated wasting syndrome
Antagonist of IIb/IIIa Receptors, preventing cross linking Used in post angioplasty and acute coronary
reaction in platelet aggregation syndromes
Blocks IL-2 receptors. Used in kidney transplants.
Used in Crohn's disease and rheumatoid arthritis,

Antibody targeted against TNF- alpha.
ankylosing spondylitis, psoriatic arthritis.
Antibody to CD3 from Tcells Used in acute renal allograft rejection.
Antibody to surface (fusion) protien of RSV Prophylaxis and treatment of RSV.
Bind to alpha-4-integrin Multiple sclerosis, crohn's disease
Bind to CD20 Used for B-cell non-hodgkins lymphoma.
Binds to HER-2 protein on surface of tumor cells (breast

Cytotoxic for breast tumors.
cancer)
Adverse effects
-
Xerosis and acneiform rash on face, upper chest and

upper back.
Highly nephrotoxic, gingival hyperplasia and hirsutism
Highly nephrotoxic
Associated with invasive CMV infections
Risk of PML in patients with JC virus infection
-
Hormone Agents
Somatotropin, somatrem (GH
analog)
Growth hormone
Somatostatin, Octreotide (GH
antagonist)
Gonadorelin, leuprolide, nafarelin,

goserelin, histrelin, triptorelin.
Gonadotropin (GnRH analogs)
releasing hormone
Ganirelix, cetrorelix, abarelix,

Degarelix. (GnRH antagonist)
Prolactin Dopamine agonist (bromocriptin)
Oxytocin Oxytocin
Vasopressin Desmopressin
MOA Indications
GH deficiency, Prader willi syndrome, turner
Released in pulsatile manner in response to syndrome idiopathic short staure, treat wasting in
GHRH
AIDS patients.
Acromegaly, gigantism, VIPoma, carcinoid

Inhibit GH secretiong from ant. Pituitary syndrome, Zonger ellison syndrome and
esophageal varices bleeding control.
Pulsatile GnRH secretion ti stimulate the Stimulation:- Male and female infertility and
gonadotropic cells to release LH and FSH. First diagnosis of LH response. Suppression in
act as agonist and in continue therapy act as Endometriosis, uterine fibrodes, prostate cancer,
anatagonist. advanced breast and ovarian cancer.
Competitive antagonist of GnRH receptors Supression of hormone release to prevent LH surge

that inhibit release of LH and FSH and in advanced prostate cancer.
Supression of prolactin release Hyperprolactinemia.
Release of oxytocin IV for intiation of labor, IM for controlling post

partum bleeding.
Released inresponse to elevated plasma DOC for central diabetes insipidus, hemophilia A,
osmolarity or hypotension von Willebrand disease, Nocturnal enuresis.
Adverse effectss
Intracranial hypertension, scoliosis, risk of otitis
media, hypothyroidism, myalgia, arthalgia, carpel
tunnel syndrome.
Symptoms of menopause hot flashes, sweat,

headache, depression, decreased libido, vaginal
dryness, osteoporosis,
Nausea, headache, light headedness, fatigue,

orthostatic hypertension.
Fetal distress, placental abruption, uterine
rupture, severe hypotension.
Hyponatremia and seizures.

Type Agents MOA
Inhibition of thyroid perioxidase and PTU
Thionamides Propylthiouracil inhibit 5-deiodinase and thus prevent
Methimazol
peripheral conversion of T4 to T3
Inhibit proteolytic cleavage of T3 and T4
Iodides Potassium iodides from thyroglobulin and inhibit thyroid
hormone release.
Anion inhibitors Perchlorate,Pertecnetate,T Block uptake of iodide

hiocynate
It causes active accumulation of iodide in

Radioactive iodine Sodium iodide I 131
thyroid gland.
Indication
Hypothyroidism. 1st trimester use PTU, 2/3rd
trimester use carbimazole or methimazole
Pretreatment for thyroid surgery.

Contraindicated in pregnancy.
Rarely used clinically
-
Adverse effects
Puritic rash, agranulocytosis, hepatotoxicity, teratogenecity
with metimazole and carbimazol
Mild skin rashes and other hypersensitivity.
Can cause aplastic anemia
Should not be administered to pregnant women or nursing

mothers, since it crosses placenta to destroy fetal thyroid
gland and is excreted in breast milk.
Types of insulin Agents
Lispro, Aspart,
Rapid acting Glulisine
Regular (Novolin and
Short acting Humulin)
Lente, NPH (Neutral
Intermediate acting protamine hagedron
or isophane)
Ultralente and insulin
Long acting glargine
Insulin detemir
Inhaled Insulin
Action and Uses
Duration of action 4-5 hrs, Peak effect is 1-2 hrs, onset is 5-20
mins. To be taken immediately before meals.
Duration of action 5-8 hrs, Peak effect is 2-4 hrs, onset is 30 mins.
Before 30-45 mins of meals
Duration of action 4-12 hrs and onset is 2-5 hrs. Peak depends on
amount of doses.
Duration of action 11-24 hrs and onset is 1-1.5 hrs, acheives

maximum effect after 4-6 hrs. It has no peak.
Duration of action is more than 24 hrs and onset is 1-2 hrs.
Duration of action is 5-10 hrs and rapid onset, primarily used
instead of short or rapid acting insulin.
Adverse effects
Hypoglycemia (lip tongue tingling, lethargy, confusion, sweats,
tremors, tachycardia, coma ,seizures. Insulin allergy immediate type
hypersensitivity with local or systemic urticaria. Severe cases
anaphylaxis.
Type Agents
First gen:-
1. Acetohexamide
2. Tolbutamide
3. Chlorpropamide
Sulfonlyureas 4. Tolazamide
Second gen:-
5. Glipizide
6. Glyburide
7. Glimepiride
Repaglinide
Meglitinide analogs
Nateglinide
Biguanides (Euglycemic) Metformin
Thiazolidinediones Pioglitazone, Rosglitazone.
α glucosidase inhibitor Acarbose, miglitol

MOA
Block K+ channels lead to depolarization and cause

insulin release. Increase the sensitiztion of insulin
receptors.
Stimulate insulin release from pancreatic beta cells

and regulate K+ channels.
Reduce hepatic production by activating

AMPkinase enzyme. Slow absorptionof glu. in GI
Bind to nuclear PPARs included in transcription of

insulin, sensatization of insulin in tissue, increase
number of GLUT4 receptors, decrease
gluconeogenesis.
Competitive Inhibitor of α glucosidase.

Adverse effects and other
Hypoglycemia, weight gain, hypersensitivity. Each

1. Decrease dose in renal dysfunction. number of
2. Short half life, safe in elderly and no problem in renal adv effect
3. Long acting contraindicated in renal and hepatic is
dysfunction. Disulfiram like reaction. according
4. Comparable to chlorpropamide. to the
5. Shortest half life contra. In renal and hepatic dysfunction. drug
6. Contraindicated in renal and hepatic insufficiency. number
Very fast onset of action, peak effect in 1 hr after ingestion,

caution in renal and hepatic dysfunction.
Safe in patient with renal dysfunction.
Most common GI distress, lactic acidosis, interfers with

vitamin B12 absorption.
Fluid retention, peripheral edema, risk of heart failure,

weight gain, bone fracture risk.
Flatulence, diarrhea, abdominal pain, contra. In IBD renal

dysfunction
Agents
Fludrocortisone (aldosterone
Mineralocorticoids
agonist)
Hydrocortisone (cortisol),
Glucocorticoids used
Triamcinolone, Betamethasone ,
topically Dexamethasone
Cortisone, Prednisone,
Other
Prednisolone, Methylprednisolone,
Inhibitors of adrenocor. MOA

Synthesis
Blocks 11 hydroxylation it is used

Metyrapone for adrenal test and in pregnant
women with cushing syndrome.
Inhibit conversion of cholesterol to

Aminoglutethimide pregnenolone
Antifungal inhibit all gonadal and
Ketoconazole
adrenal steriod synthesis.
Reversibly bind to 3 beta
Trilostane
hydroxysteroid dehydrogenase.
Indications Adrenal Indications Non adrenal
Dexmethasone for cushing Many for allergies, asthma,

syndrome, for replacement in antiemetic, carcinomas,
addison's disease, congenital thyrotoxicosis, DOC for sarcoidosis
adrenal hyperplasia (CAH) also for dematologic conditions
Others
Mifeprestone:- potent glucocorticoid

antagonist
Spironolactone, eplerenone :
Aldosterone antagonist
Adverse effects
Osteoporosis, hypothalmus-pituitary-
adrenal-axis supression, cushing like
syndrome, cataracts, psychosis, peptic ulcer,
easy brusiablity, glucose intolerance,
hyperglycemia, hypertension, edema,
hypokalemia.
Type Agents MOA
Natural estrogens Estradiol, estrone, estriol
Ethinyl estradiol, mestranol -

Synthetic estrogens (steroidal), Diethylstilbestrol
(non steroidal)
Depend on target tissue at

Tamoxifen (competitive partial Bone: Agonist,
agonist of estradiol) Breast: Antagonist, Endometrium:
Partial Agonist.
Depend on target tissue at

Bone: Agonist,
Selective estrogen Raloxifene Breast: Antagonist, Endometrium:
receptor modulators Antagonist
Decrease feedback inhibition by

blocking estrogen receptors in
Clomiphene hypothalamus pituitary by
increasing FSH and LH-> ovulation->
pregnancy
Natural progestorne Progestin
-
Synthetic Medroxyprogesterone (oral or
progesterone IM), Hydroxyprogesterone
(IM), Megestrol (oral),
norethindrone, norgestrel
Progesterone Bind strongly to progesterone

Inhibitors Mifepristone receptor.
Danazol Inhibit ovarian steroid synthesis

Other inhibitors and
antagonists.
Aromatase inhibitor -> ↓ estrogen
Anastrozole synthesis.
Combination of estrogens
Selective inhibition of pituitary function resulting in inhibiti
(Ethinyl estradiol, mestranol) ovarian function and change in cervical mucus and endome
and progesterones
(norethindrone, norgestrel) secretion.
Hormonal
Contraception
Hormonal
Contraception
Continous progesterone Affect cervical mucus and motiliy of tubes. Does not alway
Decrease risk of endometrial and ovarian CA, decrease dys
therapy without estrogens. endometriosis, pelvic inflammatory disease, osteoporosis.
Androgens Methytestosterone: Testorsterone analog

Oxadrolone, nandrolone
Non steroidal competitive inhibitor

Flutamide of testosterone receptor.
Antiandrogens Leuprolide GnRH analog

Finasteride 5-alpha reductase inhibitor
Ketoconazole Synthesis inhibitor
Clinical use Adverse effects
Replacement therapy in estrogen deficits, Nausea, breast tenderness, hyperpigmentation,
hypogonadism, birth control, dysmennorhea, uterine bleeding, increased risk og migraine
acne, prostate CA, combined with estrogen to
supress ovulation in patient with headaches, cholestasis, HTN, increased bld
coagulation by increase in factor II, VII, IX, X and
dysmennorhea, hirsuitism due to excess cancer.
androgens.
Palliative treatment of breast cancer,

prevention for expected loss of lumbar Hot flashes, N/V, risk of endometrial cancer.
density.
Prevention of post menopausal osteoporosis

and prophylaxis of breast CA.
Fertility Drug Multiple pregnancy.
Depot contraception: medroxyprogesterone

IM every 3 months, Treatment of
dysmenorrhea, endometriosis, bleeding ↑LDL and ↓HDL, glucose intolerance,
disorders, contraception, Implant: norgestrel 5 breakthrough bleeding, hirsuitism and acne.
years, hormone replacement therapy, test
estrogen secretion.
Cause breakdown of decidua leading to

detachment of blastocyst from endometrium
so used as ER postcoital contraceptive.
Endometriosis and breast fibrocystic disease, Mild hirsuitism and acne, oily skin,
Heavy menstrual bleeding, Hereditary dysmennorhea, teratogenic, hepatotoxicity,
angioedema ↓HDL.
Firstline for locally advanced or metastatic
breast cancer in postmenopausal women. -
uitary function resulting in inhibition of ovulation, depress Mild:- Nausea, headache, Moderate:
nge in cervical mucus and endometrial motlity and breakthrough bleeding, weight gain, hirsuitism,
amenorrhea, severe: vascular disorder, GI
disorders, depression. Effect is decreased in
interaction with antimicrobials and enzyme
inducers like barbiturates, phenytoin, rifampin,
carbamazepine.
Mild:- Nausea, headache, Moderate:
breakthrough bleeding, weight gain, hirsuitism,
amenorrhea, severe: vascular disorder, GI
disorders, depression. Effect is decreased in
interaction with antimicrobials and enzyme
motiliy of tubes. Does not always inhibit ovulation. inducers like barbiturates, phenytoin, rifampin,
rial and ovarian CA, decrease dysmenorrhea, carbamazepine.
ammatory disease, osteoporosis.
Male Hypogonadism, increase muscle mass, Excessive musculinization, tendone rupture,

strenght, physical performance, illict use in acne, cholecystic jaundice, agression
athelets dependence.
Used for inoperable prostate cancer -
Repository form in prostate CA -

Benign prostatic hypertrophy, male type -
baldness
In androgen receptor positive CA -
Contraindication
In estrogen dependent neoplasm,
undiagnosed genital bleeding, liver
disease, heavy smokers, pregnancy, in
uterine fibroids, thromboembolic
disorder.
Thrombophlebitis, thrombotic
phenomena, cardiovascular, asthma,
liver disease, eczema, migraine,
diabetes, HTN or convulsive disorder.
Thrombophlebitis, thrombotic
phenomena, cardiovascular, asthma,
liver disease, eczema, migraine,
diabetes, HTN or convulsive disorder.
-
-
-
Agents MOA
Calcipotriene
Doxercalciferol and Analogs of 1,25 dihydroxy
paricalcitol
Bisphosphanates Inhibition of the osteoclastic

proton pump necessary for
First gen:- Etidronate dissolution of hydroxyapatite
Second gen:- Alendronate, ↓ in osteoclastic activity
Pamidronate, Residronate.
Third gen:- Ibandronate. ↑ osteoclastic apoptosis
↓ IL-6 secretion
Recombinant PTH: Stimulate new bone formation

Teriparatide. and ↑ bone mineral density.
Calcitonin: Inhibits osteoclastic bone

Fortical, Miacalcin resorption.
Calcium side effects will be

constipation
Indication Adverse effects
Used in Psoriasis -
Secondary Hyperthyroidism in patient with
chronic kidney disease.
Postmenopausal women with vertebral compression Hypocalcemia, increased PTH, skin

fractures, in elderly men for non traumatic fracture,
secondary osteoporosis due to corticosteriods rash, upper GI irritation,
(alendronate), paget disease, cancer metastasis. Esophageal ulceration.
Given daily by subcutaneous injection in

osteoporosis.
Useful drug for treatment of Paget’s disease,

hypercalcemia, and osteoporosis.
Type Agents MOA
Thiazide Diuretics
Loop diuretics (furosemide) Lower the BP by depleting body sodium

Diuretics
stores.
K+ sparing diuretcs
Aldosterone anta.
(Spironolactone)
Methyldopa Alpha-2 agonist (decre. HR and CO)
Centrally acting Clonidine Alpha-2 agonist (bradycardia)20

sympathoplegic
Guanabenz
Guanfacine
Bind to storage granules and inhibit NE
Guanethidine
Adrenergic neuron release
blocker Bind to VMAT and depletion of NE, DA,
Reserpine
and 5HT
Alpha 1 blocking Prazosin, Doxazosin, Decrease arteriol resistance and
agents Terazosin decrease venous resistance
Beta blocking agents Propanolol
Hydralazine Release nitric oxide --> arteriolar dilation
Arteriolar vasodilation, opens K+

Minoxidil channels cause hyperpolarization
Dilates both arteries and veins,
Direct acting Sodium Nitroprusside stimulate guanyl cyclase effects
vasodilators disappear in 1-10 mins
Diazoxide Arteriolar vasodilation, opens K+

channels cause hyperpolarization
Fenoldopam Peripheral arteriol dilation, D1 agonist

Verapamil
Block Ca2+ channels decrease
Calcium channel Diltiazem contractility. Vasodilate esp. arterioles,
blockers coronary vessels and also hve natriuretic
-dipines (nefedipine) renal effects.
Angiotensin Captopril, enalapril, Hydrolyzes angi. I to II, inhibit

Converting enzymes
inhibitors (ACEIs) lisinopril metabolism of bradykinin
Angiotensin receptor Losartan, Eprosartan, Block angiotensin II but does not affect
blockers (ARBs) erbesartan, olmesartan bradykinin.
Renin Inhibitor Aliskerin Bind to active site of renin and inhibits

its effect
Indications
Mild to moderate HTN
Severe HTN
Used in preganacy HTN
Used in mild to moderate HTN and also in

dependency states such as opioids or nicotine
HTN
HTN
HTN, BPH
See adrenergic blockers
Used in moderate to severe HTN in pregnancy
Used in moderate to severe HTN and topical for

hair growth in male type baldness
DOC for emergency hypertension crisis.
Hypertensive ER, insulinoma
Used in HTN ER and postoperative HTN
Greater effects on heart, possible AV block at

high doses
Used in subacrachnoid hemorrage (Nimodipine),
prevent vasospasm
Used in moderate in HTN, also in heart failure and

after MI
Provide same benefits as ACEIs
-
Adverse effects
Edema, positive coombs test, increased prolactin
Dry mouth, severe rebound htn
Diarrhea, fluid retention, orthostatic hypotension
Sedation, depression, increased GI secretion,

extrapyramidal effects.
First dose syncope, orthostatic hypotension, urinary
incontinence.
ockers
SLE like syndrome in slow acetylators and higher dose.
Hypertrichosis, reflex tachycardia, headache, flushing,

drug induced diabetes.
Cyanide poisoning, rebound HTN.
Fluid retention, hyperglycemia due to decreased insulin

release, reflex tachycardia, excess hypotension
Reflex tachycardia, headache, flushing, increase
intraocular pressure (avoid in glaucoma)
Constipation, headache, gingival overgrowths,

proteinuria, inhibition of P-glycoprotein drug transporter
(only verapamil)
Dry cough, angioedema, hypovolemia, hypotension,

hyperkalemia, renal failure. Cn in pregnancy.
Same side effects but cough and angioedema is not seen
much
-
Type Agents MOA
Decrease preload by dialating veins,
Nitrates Nitroglycerine Activate NO--> Activate Guanyl cyclase--
> relax vascular smooth muscle
Calcium channel
blocker see antih
Beta blockers
Heart Failure
Inhibit Na+ K+ ATPase pump, increase
Cardiac Glycosides Digoxin
free Ca conc.
Beta agonist Dobutamine Inotropic effects and vasodilation

PDE-3 inhibitors Amirinone, milrinone Inhibit PDE-3
Effects
Decrease preload and increase venous
capacitance-->decrease cardiac work-->
decrease cardiac oxygen requirement, Used for
cyanide poisoning.
see antihypertensive
Increase contractility improves CO, improve

renal perfusion and diuresis.
Primarily used in acute HF

Used only for acute heart failure or severe
exacerbation of chronic heart failure
Adverse effects
Reflex tachycardia, fluid retention, Monday disease,

orthostatic hypotension, drug interaction with sildenafil
Hypercalcemia, hypermagnesium, GI tract more common site

of toxicity, hypoxia, myocarditis, renal failure, blurry yellow
vision
Thrombocytopenia (amirinone), N/V, arrhythmias.

Type Agents
Carbonic anhydrase
Acetazolamide, Dorzolamide
inhibitors
Furosemide, Bumetanide,
Loop diuretics
Torsemide, Ethacrynic acid
Hydroclorothiazide,Indapamide,
Thiazides Metolazone, Chlorothiazide,
Methylclothiazide,
Trichlomethiazide, Chlorthalidone
K+ sparing Spironolactone, Eplerenone,

Amiloride, Triamterene
Osmotic diuretics Mannitol

MOA Indications
Glaucoma, urinary alkalinization, metabolic
Inhibits CA in PCT, HCO3- losses
alkalosis, acute mountain sickness.
Acute pulmonary edema, acute hypercalcemia,
Inhibit the luminal Na+/K+/2Cl transporter
renal failure, anion OD, contra aminogly, lithuim,
in the thick ascending loop. digoxin, NSAIDs.
Inhibit the Na/Cl transporter on the

luminal membrane of the distal Widely used in hypertension and heart failure with
convoluted tubule (DCT) proven long term efficacy, nephrolithiasis,
Weak diuretics because most of the Spironolactone and Eplerenone: -

Hyperaldosteronic states: Primary (Conn’s
filtered Na+ is reabsorbed before reaching syndrome) or Secondary (evoked by heart failure,
the collecting tubules,
Aldosterone receptor antagonist hepatic cirrhosis, nephrotic syndrome, or other
conditions associated with diminished intravascular
(Spironolactone and Eplerenone), volume), HTN management, Heart failure, used in
Na+ channel blockers (Amiloride and female hirsutism, Amiloride: - Used for Lithium
Triamterene)
induced diabetes insipidus (amiloride)
Inhibits water reabsorption in the

Increase of urine volume, Reduction of intracranial
proximal convoluted tubule (PCT) (main and intraocular pressure, Facilitates elimination of
site), the thin descending limb of the loop
of Henle, and collecting ducts toxic drugs (ej. Cisplatin), Glaucoma.
Adverse effects
Hyperchloremic, metabolic acidosis, hypokalemia,
renal stones, drowsiness and paresthasias
Hypokalemic, metabolic alkalosis, hyperuricemia,
hypovolemia, hypomagnesemia, hypocalcemia,
Ototoxicity
Hypokalemic metabolic alkalosis, Hyperuricemia,

Hypercalcemia, Hyponatremia, Hypovolemia,
Hyperglycemia, Hyperlipidemia.
Hyperkalemia, Hyperchloremic, metabolic acidosis,

Gynecomastia , impotence, benign prostatic
hyperplasia (spironolactone)
Acute renal failure (Combination of triamterene with
indomethacin), Kidney stones (Triamterene),
Azotemia: increase BUN (Triamterene and Amiloride)
Nausea and vomiting, Hypovolemia, Dehydration and

hypernatremia ,Hyperkalemia
Type Agents MOA
HMG CoA Lovastatin, Dec. cholesterol synthesis, inc LDL

reductase receptor expression, dec. VLDL
inhibitors -statins synthesis
Strongly inhibits lipolysis in adipose

tissue and reduces the fatty acid
Niacin Niacin
mobilization in circulation (inhibits
intracellular lipase of adipose tissue)
Function primarily as ligands for the

nuclear transcription receptor, PPAR-
Gemfibrozil
Fibrates Fenofibrate alpha, Transcriptionally up-regulate
lipoprotein lipase (LPL), apoA-I and
apoA-II
Cholestyramine, Bind negatively charged bile acids and

Bile acid binding
resins colestipol, salts, prevent bile returning to liver, rise
colesevelam the HDL levels
Inhibitors Selective inhibitor of intestinal

intestinal Ezetimibe absorption of cholesterol, dec delivery
absorbtion of cholesterol to liver
Adverse effects Drug Interaction
Hepatotoxicity, myalgias, myopathy, Increase warfarin levels, possible

rhabdomyolysis, GI distress. toxicity with P450 inhibitors
Intense cutaneous flush and pruritus,

Hyperuricemia and gout, Impaired glucose
tolerance, hyperglycemia, Hepatotoxicity, _
Nausea and abdominal pain, GI ulcer
exacerbation
Fibrates compete with coumarin

GI distress anticoagulants for binding sites on
Lithiasis
plasma proteins, thus can
Myositis and myopathy potentiate anticoagulant activity of
Hypokalemia
Rash warfarin and sulfonylureas
hypoglycemics
GI distress, impair absorption of fat souble

vitamins and tetracyclines, phenobarbital,
digoxin, warfarin, aspirin, pravastatin, _
fluvastatin, and thiazide diuretics.
GI distress _
Pharmacokinetics
Lovastatin, simavastin are prodrug hydrolized in

GI, Fluvastatin is completely absorbed all
agents have high first pass metabolism by liver
Administered orally, converted to

nicotinamide, which is incorporated into the
cofactor NAD+
Gemfibrozil: Highly protien bound, Undergoes

entero-hepatic circulation, Half-life is 1.5 hrs,
70% eliminated through kidneys, mostly
unmodified
Fenofibrate: Pro-drug hydrolyzed completely in
the intestine, Half-life is 20 hrs, 60% is
eliminated in urine and approx. 25% in feces
Orally administered, neither absorbed nor

metabolized totally excreted in feces.
Metabolized in small intestine and liver via

glucuronide conjugation, Biliary and renal
excretion, Plasma half-life of 22 hrs
Type Agents Additional MOA
Block Muscuranic and alpha receptors. Less

Quinidine
cardiodepressant
Class IA Na+ blockers
Block fast Na+ channels,
activated state, state
dependent blockade
Increase APD and ERP Block muscuranic receptors and more
Procainamide
cardiosdepressant than Quinidine
Cardia antimuscuranic effects, cause peripheral

Disopyramide
vasoconstriction
Lidocaine Local anesthetic shorten phase 3 increase APD

Class IB Block fast Na+ Phenytoin Anti seizure
channels in their
inactivated state. Mexiletine Orally active congener of Lidocaine
Decrease APD
Tocainide Orally active congener of Lidocaine
Class IC Block Na+ Flecainide

Encainide _
channels esp. purkinge
fibers No effect on ERP
and APD Propafenone _
Decrease SA and AV nodal activity, Decrease slope

Class II Beta blockers Propanolol of phase 4 of AP in pacemakers, Reduces incidence
of sudden arrhythmic death after MI
Class III K+ blockers Complex effects block Na+, Ca2+, K+ and beta
increase APD ERP, Slow Amiodarone receptors. Prolong APD and ERP
phase 3 prolongation of
action potential
All drug induce
arrhythmias Increases APD and ERP, potent nonselective beta-
Sotalol blocker activity: decreases HR and AV nodal
conduction
Block both activated and inactivated L-type Ca2+

Class IV Ca2+ blockers Verapamil channels
Increase K+ efflux, inhibit Ca2+ current, decrease
Adenosine cAMP, decrease conduction velocity and
automacity of AV node, prolong ERP,
Miscellanous
Magnesium Mechanism unknown
Shortens RP, while prolonging ERP and diminishing

Digoxin conduction velocity in the AV node
Indications and Interactions
Used in many arrhythmias and to maintain sinus

rhythm. Hyperkalemia enhances its effects,
displace digoxin from binding sites and increase
its toxicity, oppose the effects of AchE inhibitors
in mysthenia
Used in many arrhythmias.
Used in many arrhythmias.
DOC for emergency cardiac arrhythmias, IV use.

Used in digitalis toxicity to reverse AV block
Used in chronic treatment of ventricular
arrhythmias
Used in chronic treatment of ventricular
arrhythmias
Prophylactic in ventricular tachycardia
Used primarily for supraventricular arrhythmias
Used in severe refractory suparventricular and

ventricular arrhythmias, Decreases clearance of
digoxin, phenytoin, quinidine, theophylline and
warfarin, Substrate of liver cytochrome CYP3A4
Prophylactic in life threatening ventricular

arrhythmias
More effective in atrial and ventricular

arrhythmias, Prophylactic in reentrant nodal and
atrial tachycardias
DOC for Paroxysmal supraventricular tachycardias
(PSVT) and AV nodal arrhythmias.
Digitalis induced arrhythmias In pts with torsades

de pointes even if serum mg+ is nl
Used to control ventricular response rate in atrial
fibrillation and flutter
Adverse effects
Nausea, vomiting, diarrhea are common, Symptoms of

cinchonism: blurred vision, tinnitus, headache,
disorientation, psychosis), Hypotension, Prolongation of
QRS and increase QT interval associated with syncope
(torsades de point) secondary to a reduction in CO
Reversible SLE like syndrome, dizziness, hallucination,

depression, psychosis, can cause asystole or induction of
ventricular arrhythmias, torsades de point.
Anticholinergic activity
CNS toxicity, may cause arrhythmias, least cardiotoxic of

conventional arrhythmias
Gingival hyperplasia
Pulmonary toxicity which may lead to pulmonary fibrosis
Proarrhythmogenic effects leading to increase sudden

death.
Metallic taste and constipation
Interstitial pulmonary fibrosis, GI intolerance, Tremor,

Ataxia, Thyroid dysfunction*, Liver toxicity,
Photosensitivity , Neuropathy, Muscle weakness, Blue skin
discoloration (“smurf” skin) due to iodine accumulation in
skin, Corneal deposits (visual defects)
Impotence, Depression, Torsade de pointes, AV block
GI distress, Dizziness, Flushing, Hypotension, AV block,

constipation increase PR interval
Flushing, Dyspnea or chest burning, Less common: sedation,
headache, nausea
_
Type Agents MOA
Irreversibly inhibits Cyclooxygenase -1, so inhibits
Aspirin prostaglandin synthesis and selectively inhibits
theThromboxane A2 synthesis
Ticlopidin
Inhibits ADP-induced expression and reduce
fibrinogen binding and platelet aggregation
Antiplatelet
Clopidogrel -II-
Increases intracellular cAMP by inhibiting PDE,

Dipyridamole
resulting in decreased Thromboxane A2 synthesis
monoclonal antibody against glycoprotein IIb/IIIa

Abciximab receptors on the platelets, Aggregation does not
Gp IIb/IIIa receptor occur.
inhibitor
Eptifibatide, Tirofiban Competitive, reversible inhibitors of fibrinogen

binding to GP IIb/IIIa receptors
Inhibits the hepatic synthesis of clotting factors ( II,

VII, IX, X), blocks gama-carboxylation of protein S
Warfarin (Oral)
Substrate for Cyt 2C9 and C also inhibits vitamin K reductase enzyme i.e
antagonist of vit. K, inhibit hepatic epoxide
reductase
Anticoagulants
It cataylzes the binding of antithrombin III to

Heparin (IV, SC) factors IIa,Ixa, Xa, XIa, XIIa resulting in their rapid
inactivation
Rapidly lyze thrombi by catalyzing the formation of

plasmin from its precursor plasminogen, Plasmin
Fibrinolytic Streptokinase, Urokinase
degrades fibrin and fibrinogen, thus causing clot
dissolution
AMINOCAPROIC ACID – by competitively blocking plasminogen

TRANEXAMIC ACID: also antifibrinolytic agent
Indication
Prevention of arterial thrombosis in patients
with IHD (ischemic heart disease) and stroke
(primary indication), Angina, TIA, MI
Prevention of thrombotic stroke, Intermittent

claudications, Atrio-ventricular shunts, Open
heart surgery
-II-
Combined with aspirin to prevent cerebral

ischemia and prophylactic to angina, combined
with warfarin for prophylactic in thromboemboli
in pts with prosthetic valves.
Used along with Heparin or Aspirin during

percutaneous transluminal coronary
angiography/angioplasty for prevention of
cardiac ischemic complications
-II-
Deep vein thrombosis, Extension of established

deep vein thrombosis, Thrombosis and
embolisation in patients with atrial fibrillation,
Thrombosis on prosthetic heart valves
Rapid anticoagulation for thrombosis, emboli,

unstable angina, disseminated intravascular
coagulation, open heart surgery, etc safe in
pregnancy.
Pulmonary thromboembolism, Deep venous

thrombosis, Stroke due to thrombosis in the
major cerebral vessel/ carotid arteries, Post- MI
blocking plasminogen activation, it inhibits fibrinolysis,

gent
Adverse effects
Bleeding, Gastric irritation , Gastric ulcers, Bleeding
from the gastric ulcers
Neutropenia/Agranulocytosis, Thrombotic
Thrombocytopenic purpura (TTP), Aplastic anemia, Rash,
Diarrhea, Nausea, Dyspepsia, inhibit cytp450
Rarely asscociated with neutropenia
Bleeding, Thrombocytopenia, Hypotension, Bradycardia
Bleeding
Bleeding, Fetal hemorrhage and teratogenicity if given

during pregnancy (Fetal warfarin syndrome): serious
birth defect characterized by abnormal bone formation,
contra. Pregnancy, Aneurysm, Recent surgery,
Hypersensitivity, Skin Necrosis *
Bleeding, osteoporosis, heparin induced

thrombocytopenia (use Argatroban), hypersensitivity
(type II)
Hemorrhage especially intracranial, Arrhythmias,

Streptokinase: can cause hypersensitivity reactions, so
should not be repeated frequently

Drugs

Uploaded by

Document Information

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Drugs

Uploaded by

Copyright:

Available Formats

Disease Type

Down's Syndrome Trisomy 21

Anti Histamine Diphenhydramine (Benadryl)

Salicyclic acid Irreversible Inactivates COX; Forms irreversible covalent bonds w/

COX-2 selective inhibition

Binds to intracellular protein tubulin-> dec. microtubular polymerization-> inhibit leukocyte m

1st gen Antihistamine

Potent anti-inflammatory, anti-pyretic, analgesic

Anti-pyretic (CNS);Weak Anti-inflammatory

ular polymerization-> inhibit leukocyte migration & phagocytosis

00mg); Anti-inflammatory (3-6g); Hyperventilation & Resp. Alkalosis (6-10g); Dehy

Tx of Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis

Tx of Oosteoarthritis & Rheumatoid arthritis

Hyperuricemia; Uricosuria; Gastritis, ulcers, HSR, Gastric Lavage; HCO3 (IV)

of PDA, Thromocytopenia, Aplastic anemia

Cross allergic w/ Sulfonamides; HTN

Eicosanoids Misoprostol (PGE1)

Eicosanoids Dinoprostone (PGE2)

Eicosanoids Carboprost (PGF2a)

Eicosanoids LTA4, LTC4, LTD4

Protection of Gastric mucosa; Uterine contractions Tx of NSAID induced ulcers

Uterine SM contractions; used for cervical ripening; also as an

Reversible non-selective COX

NSAIDs Indomethacin Propionic acid Inhibits synthesis of PGs

NSAIDs Etodolac Acetic acid

NSAIDs Piroxicam Oxicam

relatively COX-2 inhibitor at

NSAIDs Ketorolac used parenterally (IV or IM)

NSAIDs Celecoxib COX-2 selective inhibition

NSAIDs Valdecoxib COX-2 selective inhibition

NSAIDs Rofecoxib COX-2 selective inhibition

Inhibitis COX in CNS; peripheral

Analgesic, Antipyretic, anti-inflammatory

Analgesic, Antipyretic, anti-inflammatory

Tx of Acute Gouty arthritis,

Tx of Oosteoarthritis & Cross allergic w/

Risks for Toxic epidermal

Hepatic toxicity; Renal tubular

Chr. Gout Allopurinol

Chr. Gout Probenecid

Chr. Gout Sulfinpyrazone

Chr. Gout Febuxostat

Non-purine, potent & selective inhibitor of Xanthine oxidase

GI distress, Rash, Nephritic syn., Crystallization

GI distress, Rash, Nephritic syn., Crystallization

Anti Histamine Cyclizine (Marezine) 1st gen Antihistamine

Stronger sedative effects

NO or less sedative effect

serotonin Olanzapine antagonist of 5HT 2A (atypical

serotonin Ondansetron antagonist of 5HT 3

Decrease negative symptoms of psychosis

Carcinoid syndrome, GI tumors

Prodrome for migraine attacks

Prophylatic in migraine, used ass substitute for LSD

Non BZs MOA

Buspiron 5HT1a partial agonist

Sleep-onset as well as sleep maintenance insomnia

Anxiety and panic attacks, IV in status epilepticus

Non sedating, indicated for generalized anxiety

High to very high

Generalized-onset and focal-

Long acting opiod receptor

Weak NMDA receptor antagonist

Fomipezole Inhibit alcohol dehydrogenase