You are on page 1of 56

MAPS

DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Adrenergic Drugs


SYMPATHOMIMETICS/ ADRENERGIC AGONISTS

DIRECT-ACTING INDIRECT-ACTING
BETA Agonists Reuptake
Non-Selective ALPHA Agonists DOPAMINE Agonists Releasers Inhibitors
(Catecholamines)

NON-SELECTIVE BETA-1 BETA-2 DOPAMINE-1 DOPAMINE-2 Tyramine


ALPHA-1 ALPHA-2 TCAs
Epinephrine
Fenoldopam Bromocriptine Ephedrine
SABAs LABAs ULABAs
Apraclonidine Dobutamine Tocolytics
Phenylephrine Isoproterenol Cocaine
= Glaucoma
Norepinephrine Cabergoline
Salbutamol/ Amphetamine
Salmeterol Indacaterol
Albuterol Ritodrine
Methoxamine Brimonidine =
Glaucoma Atomoxetine
Dopamine Methamphetamine
Formoterol Olodaterol
Terbutaline
Isoxsuprine
Tetrahydrozoline Clonidine = Anti-
HTN Bambuterol Vilanterol Phenmetrazine Sibutramine
Metaproterenol

Methyldopa = Anti- Methylphenidate


Oxymetazoline
HTN Pirbuterol
Modafinil
Propylhexedrine Guanfacine = Anti-
HTN
MIXED-ACTING
Phentermine
Ephedrine
Naphazoline Guanabenz = Anti-HTN
Angiotensin
Mephentermine II
Dexmedetomidine = IV sedative

Metaraminol

Phenylpropanolamine

Pseudoephedrine
DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Adrenergic Drugs
SYMPATHOLYTICS/ ADRENERGIC ANTAGONISTS

DIRECT-ACTING

With Intrinsic
With Membrane-
ALPHA Stabilizing Action With Mixed Alpha-1 and Enhances
BETA BLOCKERS Sympathomimetic
BLOCKERS (MSA) Beta Blocking Activity Nitric Oxide
Activity (ISAs)

Propranolol
CARDIOSELETIVE Carteolol Carvedilol Nebivolol
NON-SELECTIVE ALPHA-1 ALPHA-2 NON-SELECTIVE (BETA-1 BLOCKERS)
BETA BLOCKERS
Pindolol
Celiprolol Labetalol
Metoprolol
Phenoxybenzamine = Prazosin = Anti-HTN Yohimbine
IRREVERSIBLE Nadolol
Acebutolol
Labetalol
Celiprolol

Doxazosin = Anti- Sotalol


Phentolamine = Rauwolscine Labetalol
REVERSIBLE HTN Acebutolol
Bisoprolol
Timolol Peripherally-acting
Metoprolol
Terazosin = Anti- Penbutolol
Betaxolol
HTN
Pindolol Tyrosine
Pindolol Release Storage
Esmolol Hydroxylase
Tamsulosin = Inhibitors Inhibitor
Inhibitor
Anti-BPH Propranolol

Atenolol
Metyrosine Guanadrel Reserpine
Alfuzosin = Anti-
BPH
Acebutalol

Guanethidine
Nebivolol

Bretylium
DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Cholinergic Drugs
CHOLINOMIMETICS/ CHOLINERGIC AGONISTS
DIRECT-ACTING INDIRECT-ACTING
(AChE inhibitors)
CHOLINE
ALKALOIDS
ESTERS
Aminoalcohols Carbamates Organophosphates
Non-selective Muscarinic- Muscarinic- Nicotinic- (Short-Acting) (Intermediate-Acting) (Irreversible, Long-Acting)
Non-selective
Choline Esters selective Selective Selective

Tx for Carbamate
Bethanechol Edrophonium Malathion
Acetylcholine Arecoline Muscarine Nicotine Myasthenia Gravis Insecticides
(Urecholine)

Physostigmine/Eserine Carbaryl Parathion


Carbachol Pilocarpine Lobeline

Nerve Gases
Methacholine Varenicline Neostigmine Aldicarb
(Sarin, Tabun, Soman)

Pyridostigmine Carbofuran Echothiphate


CENTRALLY-ACTING
(Anti-Alzheimer’s)
Ambenonium Oxamyl

Tacrine
Demecarium Methomyl
Donepezil

Galantamine

Rivastigmine
DRUGS FOR AUTONOMIC NERVOUS SYSTEM: Cholinergic Drugs
CHOLINOLYTICS/ CHOLINERGIC ANTAGONISTS
ANTIMUSCARINIC/ANTICHOLINERGIC AGENTS
NON-SELECTIVE
CNS-Acting Ophthalmic Respiratory Gastric GIT and Urinary
Atropine Antimuscarinics Antimuscarinics Antimuscarinics Anticholinergics Anticholinergics
Choline
Vesicular Uptake Exocytosis Cholinesterase
Reuptake
Inhibitor Inhibitor Reactivators
Inhibitor
Scopolamine Homatropine Ipratropium Pirenzepine Methscopolamine

Hemicholinium Vesamicol Botulinum Pralidoxime


Biperiden Anistropine Tiotropium Telenzepine Glycopyrrolate

Diacetyl
Monoxime
Benztropine Cyclopentolate Oxitropium Propantheline Hyoscine

ANTI-NICOTINIC AGENTS
Ganglionic Blockers Neuromuscular Blockers Trihexyphenidyl Tropicamide Dicyclomine Dicycloverine
(NN Blockers) (NM Blockers)

Depolarizing, Irreversible, Nondepolarizing,


Hexamethonium Oxybutynin
Noncompetitive Reversible, Competitive

Succinylcholine/ Steroidal Derivatives


Trimethaphan Isoquinoline Derivatives
Suxamethonium Scopolamine

Mecamylamine Tubocurarine Rocuronium

Atracurium Pancuronium

Cisatracurium Vecuronium
AUTACOIDS: Bradykinin, Eicosanoids, Serotonin, Histamine
BRADYKININ SEROTONIN
Receptor Location Effect Drugs

EICOSANOIDS: Prostaglandin Analogues 5-HT 1A CNS (pre-


synaptic)
↓ release of 5HT (inhibitory
effect)
Buspirone (partial; anxiolytic)

Drug PG Effect Use 5-HT 1B/1D Cerebral cerebral vasoconstriction -triptans (migraine headache)
Type blood (anti-migraine effect)
Misoprostol PGE-1 Cytoprotection •NSAID-induced ulcer Vessels
•Opening of Ductus Arteriosus
5-HT 2A/2B Smooth contraction of smooth Ergotamine (migraine headache)
Epoprostenol PGI-2 Vasodilation •Primary Pulmonary HTN muscles muscles Ergonovine (post-partum bleeding)
•Oxytosis (uterine Methysergide (prophylaxis of migraine)
contraction; opposite of Ketanserin (anti-HTN)
Dinoprostone PGE-2 Cervical •US-approved abortificacient tocolysis)
ripening •Bronchospasm
•Vasoconstriction Ritanserin (inhibit platelet aggregation)
Alprostadil PGE-1 Vasodilation (in •Erectile Dysfunction (male- Platelets
local penile assited suppository) Platelet aggregation
tissue)
5-HT 3 Chemorecept Emesis -setrons (Chemotherapu-induced N&V)
Latanoprost PGF-2α Reduced •Glaucoma or Trigger *Alosetron ( IBS-diarrhea)
(also intraocular *Off-label: eyelash growth Zone (CTZ)
Carboprost) pressure enhancer
5-HT 4 GI Tract Peristalsis Cisapride (partial)
Tegaserod (partial)
Prucalopride
^^ IBS-constipation

NOTE: Ergot Alkaloids are NOT autacoids. They only act on 5-HT receptors.
ERGOT ALKALOIDS:
1. Alpha Agonists = Methylergonovine
2. Alpha and 5-HT Agonist = Ergotamine
3. 5-HT Agonists = Methysergide
4. Other Alkaloids
1. Bromocriptine
2. Cabergoline
3. Perfgolide
4. Ergonovine
AUTACOIDS: Bradykinin, Eicosanoids, Serotonin, Histamine
HISTAMINE
AGONISTS ANTAGONISTS

Histamine (Exogenous) Pharmacologic


Functional
(Antihistamines)
Betahistine

Epinephrine H1 Antihistamines H2
Impromidine Antihistamines

Second
First Generation Cimetidine
Generation

Ethanolamine Ethylenediammine Alkylamine Piperazine Phenothiazine Piperidine Piperazine Piperidine Alkylamine Newer Agents Famotidine

Pyrilamine/
Diphenhydramine Chlorpheniramine Meclizine Promethazine Cyproheptadine Cetirizine Loratadine Acrivastine Bilastine Ranitidine
Mepyramine

Dimenhydrainte Tripelenamine Brompheniramine Cyclizine Levocetirizine Desloratadine Ebastine Nizatidine

Doxylamine Hydroxyzine Fexofenadine

Astemizole
Carbinoxamine
(withdrawn)

Orphenadrine
DRUGS FOR RHEUMATOLOGIC DISORDERS
ANALGESICS: NON-NARCOTICS
Paracetamol NSAIDs

Non-Selective Specific COX-2


COX Inhibitors Inhibitors

Salicylic Acid Pyrazolone Indole Pyrrole Alkanoic True Phenyl Acetic Acid Oxicam Propionic Acid
Fenamates Celecoxib
Derivatives Derivatives Derivatives Acid Derivatives Acetates Derivatices Derivatives Derivatives

Aspirin Phenylbutazone Indomethacin Tolmetin Sulindac Ketorolac Mefenamic Acid Piroxicam Ibuprofen Etoricoxib

Meloxicam**
Diflunisal Dipyrone Aceclofenac Etodolac Meclofenamic Acid (preferentially Naproxen Parecoxib
selective to COX-2)

Magnesium Choline
Sulfinpyrazone Diclofenac Nabumetone Flufenamic Acid Keptoprofen Valdecoxib
Salicylates

Rofecoxib
Methyl Salicylate Flurbiprofen
(withdrawn)

Meloxicam **
(preferentially
selective to COX-2)
DRUGS FOR RHEUMATOLOGIC DISORDERS
ANALGESICS: NARCOTICS
OPIOID AGONISTS

Opiates Semi-synthetic Opioids Opioids (BY ACTIVITY)

Semisynthetic Semisynthetic Strong Full


Morphine Heroin Apomorphine Morphine Codeine Mild-to-moderate Partial
Derivatives Derivatives Agonists Agonist Agonists

Codeine Hydromorphone Hydrocodone Morphine Codeine Nalbuphine

Thebaine Oxymorphone Oxycodone Heroin Hydroxycodone Butorphanol

Hydroxymorphone Tramadol Buprenorphine


OPIOID ANTAGONISTS
Naloxone Methadone Pentazocine

Naltrexone

Meperidine
Nalorphine

Nalmefene
Levorphanol
Levallorphan

Fentanyl
DRUGS FOR RHEUMATOLOGIC DISORDERS
DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDs)

NON-BIOLOGICALS

Methotrexate Antimalarials Leflunomide Mycophenolate Gold Compounds


Sulfsalazine (active metabolites)
(A77 1726) Mofetil

Chloroquine Aurothiomalate

Sulfpyridine
Hydroxychloroquine Auroglucose

5-aminosalicylate/
mesalamine Auranofin

BIOLOGICALS

T-cell Activation B-cell Depleting


IL-6 Inhibbitor IL-1 Neutralizer TNF-a Inhibitors
Inhibitor Agent
GLUCOCORTICOIDS

Abatacept Rituximab Tocilizumab Anakinra Adalimumab

Prednisone Methylprednisone Dexamethasone

Infliximab
*Route of Administration of Glucocorticoids:
•Systematic (IV, PO) = RA, SLE
•Local (Intrasynovial) = Osteoarthritis
Etanercept
DRUGS FOR RHEUMATOLOGIC DISORDERS
DRUGS FOR GOUT

ACUTE GOUT CHRONIC GOUT


Drug MOA NOTES T/E Drug MOA NOTES

st st
Colchicine Inhibits polymerization of 1 line for ACUTE Gout •Watery Allopurinol Inhibits Xanthine Oxidase/ 1 line for CHRONIC Gout
tubulin  inhibition of diarrhea Xathine Oxidoreductase Purine analog
microtuble synthesis •Bloody
diarrhea
•Neuropathy
Febuxostat Inhibits Xanthine Oxidase/ Non-purine
Xathine Oxidoreductase
NSAIDs COX inhibition Indomethacin (Topical) -[recall
Ibuprofen NSAIDs S/E)
Pegloticase, Anti-inflammatory Uricase = not present In
*Do NOT give Aspirin, Rasburicase immunosupression mammals, converts uric acid to
Tolmetin, and Salicylates ALLANTOIIN (non-toxic
metabolite)
Glucocorticoids Anti-inflammatory Used NOT MORE THAN 5 •Cushing
immunosupression DAYS syndrome Penicillamine Enhance urinary secretion RISK: formation of RENAL
(especially if non-responsive Probenecid of uric acid (uricosuric URIC ACID STONES
to Colchicine and NSAIDs) Sulfinpyrazone agents)  prevention: frequent
hydration
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR COAGULATION DISORDERS: Anti-thrombotics
ANTICOAGULANTS
DIRECT INDIRECT
ANTICOAGULANTS ANTICOAGULANTS

PARENTERAL ORAL PARENTERAL ORAL

Hirudin Unfractionated Low Molecular


Dabigatran Heparin Weight Heparin Xa inhibitors
Coumarin
Derivatives

Enoxaparin Dicoumarol
Lepirudin Apixaban
(withdrawn)

Dalteparin Phenprocoumon
Rivaroxaban
Bivalirudin (withdrawn)

Tinzaparin
Warfarin**
Argatroban
Fondaparinux
Photo Credit: Sir Crisfel Del Mundo

Danaproid
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR COAGULATION DISORDERS: Anti-thrombotics

ANTIPLATELETS

TXA-2 Synthesis Inhibitor ADP Inhibitors PDE Inhibitors GP-IIb/IIIa Inhibitors

Irreversible Reversible
Aspirin Dipyridamole
Epitifibatide

Ticlopidine Tigacrelor
Cilostazol
Abciximab

Clopidogrel
Tirofiban

Prasugrel
DRUGS FOR HEMATOLOGIC DISORDERS

DRUGS FOR COAGULATION DISORDERS: Fibrinolytics DRUGS FOR COAGULATION DISORDERS: Pro-thrombotics

FIBRINOLYTICS/
PRO-THROMBOTICS
THROMBOLYTICS

Tranexamic Acid Vitamin K E-aminocaproic Acid Aprotinin


Tissue Urokinase
Streptokinase Anistreplase Plasminogen
Activators
K1 = Phytonadione
Alteplase

Reteplase K2 = Menaquinone

K3 = Menadione
DRUGS FOR HEMATOLOGIC DISORDERS
DRUGS FOR DYSLIPIDEMIA

Drugs for DYSLIPIDEMIA

HMG-CoA Reductase Sterol Absorption


Nicotinic Acid Fibric Acid Bile Acid Binding Inhibitor (NPCL1
Inhibitors (-statins) Derivatives/ Fibrates Resins Transporter Inhibitor)

•Most effective:
Atorvastatin increase HDL levels
Fenofibrate Ezetimibe
•T/E: Cholestyramine
Erythema/Flushing (Tx:
ASA, Ibuprofen)
•COMB. Prep:
Simvastatin +
Rosuvastatin Clofibrate Colestipol Ezetimibe (Vytorin)

Simvastatin Gemfibrozil Colesevelam

1st line: hypercholesterolemia •PPAR-Alpha Agonists


•Also used as Tx for
•1st line:
oral poisoning
hypertriglyceridemia
(Warfarin, Digitoxin)
•Do not take with
STATINS
(rhabdomyolysis)
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR PSYCHOSIS
SECOND GENERATION

Clozapine
FIRST GENERATION

Olanzapine

Loxapine

Phenothiazines Butyrophenones Thioxanthenes


Risperidone

Poliperidone
-peridol -thix

Ziprasidone
Aliphatic Piperazine Piperidine

Molindone

-promazine -phenazine -ridazine


Amisulpride

Aripiprazole

Quetiapine
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR MOOD DISORDERS: Depression, Bipolar Disorder

ANTIDEPRESSANTS

Non-selective Atypical Selective Serotonin Serotonin-NE Reversible NE-Dopamine


Tricyclic Antidepressant Tetracyclic Antidepressants Noradrenergic and Inhibitor of Noradrenaline
MAO inhibitors Reuptake Inhibitors Reuptake Reuptake Inhibitor Reuptake
Antidepressants Selective Serotonin MAO-A
Inhibitors Inhibitor
Antidepressant

Secondary Tertiary Trazodone


Amine Amine Mianserin Moclobemide Fluoxetine
Moclobemide Reboxetine
Duloxetine Bupropion
Mirtazapine

-tryptiline -pramine Maprotiline Nefazodone Fluvoxamine


Phenelzine
Venlafaxine

Desipramine Amitryptiline Amoxapine Drugs for MANIA/


Isocarboxaid Paroxetine
Resvenlafaxine
BIPOLAR DISORDER

Tranylcypramine Sertraline
Lithium Valproic
Carbamazepine Antipsychotics
Carbonate Acid

Selegiline Citalopram

Escitalopram
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR ANXIETY

Drugs for ANXIETY

Benzodiazepines Barbiturates Other Sedative-


Hypnotics

Short- Intermediate- Long- BZDs without Short- Intermediate- Long- Zolpidem


Acting Acting Acting Active Metabolites Active Ultra Short- Acting Acting Acting
of BZDs Acting
Metabolites
Zaleplon
Midazolam Lorazepam Diazepam Pentabarbital Amobarbital Phenobarbital
Clonazepam Thiopental
Nordiazepam
Triazolam Eszopiclone
Temazepam Thiamylal Hexobarbital Butabarbital Barbital
Oxazepam Oxazepam
Buspirone
Methohexital Secobarbital
Oxazepam Lorazepam

Ramelteon
Alprazolam
Alprazolam
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR SEIZURE
DRUG MOA T/E Notes
Carbamezepine Na Channel •T/E: Dose-related •DOC for
blocker Ataxia = loss of control of movement Trigeminal
Diplopia= loss of vision Neuralgia
ANTI-SEIZURE/ •Teratogenic (Spina Bifida) •Enzyme
inducer
ANTICONVULSANTS •Capable of
auto-induction
Phenytoin Blocks Na, K, •Most Common: Nystagmus •Fosphenytoin
Generalized Absence Atonic Myoclonic Status Acute and Ca •Dose-related (given as IM
Seizure Seizure Seizure Seizure Epilepticus Seizure conductance Ataxia = loss of control of movement and IV)
Diplopia= loss of vision
•Cosmetic Changes
Valproic Ethosuximide Clonazepam Lorazepam Diazepam Gingival hyperplasia, Hirsutism
Valproic •Idiosyncratic
Acid Acid SJS, Blood dyscrasias
•Teratogenic: Fetal Hydantoin Syndrome
Valproic acid Valproic Clonazepam
Topiramate Acid Valproic Acid •Increases •Hepatoxicity (avoid in <2 yrs old) •Enzyme
(more recent)
GABA •Teratogenic: Spina bifida) inhibitor
concentration
by stimulating
Topiramate
Glutamic Acid
Lamotrigine decarboxylase
•Blocks Na and
Ca conductance
Lamotrigine
Lamotrigine Na channel
blocker
Ethosuximide T-type Ca
Channel blocker

Topiramate Na and Ca
channels
blocker
DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR PARKINSON’S DISEASE

ANTI-PARKINSONIAN DRUGS

Selective MAO-B Centrally-Acting


Levodopa COMT Inhibitors D2 Agonists Amantadine Apomorphine
Inhibitors Anticholinergics

Non-Ergot
Tolcapone Selegiline Ergot Derivatives Biperiden
Derivatives

Entacapone Rasegiline Bromocriptine Pramiprexole Benztropine

Cabergoline Ropinirole Trihexyphenidyl


DRUGS FOR CENTRAL NERVOUS SYSTEM
DRUGS FOR ANESTHESIA

ANESTHETICS

General Local
Anesthetics Anesthetics

Amide Type Ester Type


Inhalational Intravenous
( Two I’s ) (One “I”)
Ultra Short- Opioid Muscle Combined
Desflurane Short-Acting Propofol Ketamine Etomidate Lidocaine/
Acting Analgesics Relaxants Therapies Cocaine
BZDs Xylocaine
Barbiturates (adjunct) (adjunct)

Sevoflurane Neurolept analgesia Prilocaine Procaine


Thiopental Midazolam Morphine Neuromuscular (Droperidol +
Blockers Fentanyl)
Isoflurane Fentanyl Bupivacaine
Thiamylal
Neurolept
Enflurane Anesthesia
Sulfentanyl (Droperidol +
Methohexital Fentanyl + N2O)

Halothane

Methoxyflurane
DRUGS FOR RESPIRATORY DISORDERS
DRUGS FOR COLDS DRUGS FOR COUGH

Drugs for COLDS Drugs for COUGH

Mucoregulators Mucolytic Antitussives Expectorant


Common Colds Allergic Colds

Ambroxol N-Acetylcysteine Opioid


Non-Narcotic Guaifenesin
Nasal Decongestants Derivatives
Antihistamine +
(Alpha-1 Agonists) Nasal Decongestants

Bromhexine Butamirate
Codeine
Citrate

Carbocisteine Noscapine

Dextromethorphan
DRUGS FOR RESPIRATORY DISORDERS
DRUGS FOR BRONCHOSPASTIC DISEASES
BRONCHODILATORS

MAST CELL STABILIZERS


Beta-2 Agonists Methylxanthines Anti-muscarinics

SABA LABAs Controller Reliever SAMA LAMA

Albuterol/ Theophylline Aminophylline


Cromolyn sodium Nedocromil
Salmeterol Ipratropium
Salbutamol (PO) (IV) Tiotropium
Bromide

Terbutaline Formoterol
ANTI-INFLAMMATORY

Metoproterenol
Anti-Leukotrienes Corticosteroids Anti-IgE

Picaterol/
Pirbuterol LTD-4 receptor Inhaled Systemic ORAL Systemic
LOX inhibitor PARENTERAL Omalizumab
Antagonists Corticosteroids Corticosteroids
Corticosteroids

Zileuton Zafirlukast Budesonide Prednisone


Hydrocortisone IV

Montelukast Fluticasone Prednisolone


Methylprednisolone IV

Triamcinolone Methylprednisolone
ENDOCRINE DRUGS
HYPOTHALAMIC AND ANTERIOR PITUITARY GLAND HORMONES AND AGENTS

GROWTH HORMONE
GONADOTROPIN RH
GH Deficiency GH Excess

Growth GH-receptor D2 Receptor Agonists (-relin) Antagonists (-relix)


Hormone Alternatives Somatostatin and Antagonist Agonist
Analogues
Cadaveric GHRH Gonadorelin Degarelix
Insulin-like Pegvisomant Bromocriptine
(obsolete) Analogue
Growth Factor-1
Analogues Octreolide

Recombinant GH Sermorelin Cabergoline Cetrorelix


Goserelin
(Somatrem) Mecasermin (for hypothalamic Lanreotide
defect only)
Ganirelix
Mecasermin Boserelin
Rinfabate
PROLACTIN
Aborelix
Leuprolide
D2 Agonist
GnRH Analogues
•Intermittent Administration (Pulsatile Dosing)
•Sustained Administration (Continuous Dosing/ IM Depot)
Long-term Mgt If pregnancy is desired

Cabergoline Bromocriptine
ENDOCRINE DRUGS

POSTERIOR PITUITARY HORMONES

OXYTOCIN VASOPRESSIN

Vasopressin Deficiency Vasopressin Excess


(Diabetes Insipidus) (SIADH)
Nasal Spray IV Infusion

Vasopressor
Central DI Nephrogenic DI Demeclocycline Receptor
To stimulate milk let-down Tx/Prevention of post- Antagonists
partum hemorrhage

Vasopressin 1st Line: Thiazide Conivaptan


Diuretics
Labor induction (1 hr
infusion only)
Desmopressin Alt: Indomethacin Tolvaptan
ENDOCRINE DRUGS

THYROID HORMONES

THYROID HORMONES

HYPOthyroidism HYPERthyroidism

Liothyronine Inorganic Radioactive Other Anti-


Thionamides Anions Iodides
(LT3) Iodine thyroid agents

Levothyroxine Propylthiouracil Potassium Strong Iodine I-131 Radiocontrast


(LT4) perchlorate Solution (Lugol’s Beta blockers Glucocorticoids
Dyes
Solution) (therapeutic)

Methimazole Sodium Iopanoic


thiocyanate I-125 Propanolol Dexamethasone Acid
Saturated Solution
of KI (KISS) (diagnostic)

Carvedilol Ipodate
ENDOCRINE DRUGS

ADRENOCORTICAL HORMONES

ADRENOCORTICAL HORMONES

Glucocorticoids Mineralocorticoids

Short-Acting Intermediate- Long-Acting (>35


(<12 hrs) Acting (12-36 hrs) Fludrocortisone Desoxycortisone
Aldosterone Antagonists
hrs)
Cortisone Paramethasone Betamethasone
Hydrocortisone Fluprednisolone Beclamethasone
Prednisone Triamcinolone Spironolactone

Eplerenone
ENDOCRINE DRUGS

GONADAL HORMONES

ESTROGEN PROGESTIN

Natural Synthetic
Endogenous 19- 19-Ethyl-19-
Progesterone
form: Testosterone Nortestosterone Nortestosterone
Derivative
Progesterone Derivatives Derivatives
E1: Estrone Steroidal Non-Steroidal
Methoxyprogesterone
acetate ( IM Depo-
Provera) Dimethylsterone Levonorgestrel Desogestrel

Mestranol Diethylstilbestrol
E2: Estradiol (Major (banned)
secretory form)
Norethindrone Norgestimate

Ethinyl Estradiol Chlorotrianisene


E3: Estriol

Quinestrol Methallenestril
ENDOCRINE DRUGS

GONADAL HORMONES
DRUGS FOR
CONTRACEPTION FERTILITY DRUGS

Combined Oral Progestin Only Emergency Contraceptives Beta-HCG (B-Human Menopausal


Contraceptives
Clomiphene Citrate Chorionic Gonadotropin) = Gonadotropins
add-on to clomiphene = add-on to clomiphene
Minipills Ethinyl Estradiol +
Ethinyl Estradiol + Levonorgestrel
Progestin Menotropins (FSH + LH)

Injectables: IM Depo-
provera)
Monophasic TESTOSTERONE Urofollitropins (FSH)

Intradermal implants
Biphasic Etonorgestrel (Implanon) Testosterone Analogues Testosterone
(Anabolic Steroids) Antagonists

Intrauterine Device (IUD): Androgen


Triphasic 5-alpha-reductase
Levonorgestrel (Mirena) Receptor
Nandrolone Inhibitors
Blockers

Finasteride Flutamide
Danazol

Bicalutamide
ENDOCRINE DRUGS

DRUGS FOR DIABETES MELLITUS

INSULIN

Based on SOURCE Based on Based on


STRUCTURE Based on USE
DURATION

Recombinant Modified Insulins


Animal-sourced Native Insulins Demand Ultra- Short/ Intermediate Long -Acting
(less immunogenic) (the rest) Basal Insulins
Insulins Rapid Rapid-Acting Acting

•Lispro •Regular •Isophane/ •Ultralente


Bovine •Aspart Insulin/ Semi- NPH •Determir
Regular Insulin Short-Acting Intermediate- •Glulisine lente/ Human •Lente •Glargine
Agents Acting Insulin •Protamine •Degludec
Lispro
Porcine •NOTE: Only •Protamine •^^peakless
NPH/Isophane insulin that is Aspart insulin
Long-Acting IV-
Insulin
administered

Insulin Zinc
Suspension
ENDOCRINE DRUGS

DRUGS FOR DIABETES MELLITUS

ORAL ANTIDIABETIC DRUGS

Insulin Amylin Alpha- Incretin SGLT-2


Biguanides Thiazolidinediones Glucosidase
Secretagogues Analogue Mimetics Inhibitors
Inhibitors

Metformin Pioglitazone Pramlintide GLP-1 Agonists DPP IV Canagliflozin


Sulfonylureas Meglitinides (SQ) Acarbose (SQ) Inhibitors
(Euglycemic= no
hypoglycemia)
Second Rosiglitazone Dapagliflozin
First Generation Repaglinide Exenatide Sitagliptin
Generation Voglibose
Phenformin
(D/C) •PPAR-Gamma
Chlorpropamide Gliclazide Agonists Liraglutide Linagliptin Empagliflozin
Nateglinide Miglitol

Tolbutamide Glipizide Dulaglitide Vildagliptin


Mitiglinide

Tolazamide Glimepiride Semaglutide


(Ozempic)

Glibenclamide/
Acetohexamide
Glyburide
DRUGS FOR CARDIOVASCULAR DISEASES: Hypertension
DIURETICS
NATRIURETICS AQUARETIC

Carbonic Anhydrase Loop/ High- Potassium-


Thiazides Mannitol
Inhibitors Ceiling Sparing

Acetazolamide True Thiazides/ Epithelial Sodium


Sulfonamides Sulfonylureas Phenoxyacetate Thiazide-like Aldosterone
Benzothiadiazides Channel (ENaC)
Antagonists
Inhibitors
Furosemide Ethacrynic
Brinzolamide Torsemide HCTZ Chlorthalidone
Acid Spironolactone Amiloride

Bumetanide
Chlorothiazide Indapammide
Dorzolamide Eplerenone Triamterene

Metolazone
Dichorphenamide
CLASS SITE OF ACTION MOA T/E
Carbonic Anhydrase Proximal Convoluted Inhibits Carbonic Anhydrase •Metabolic acidosis ( due to increase carbonic acid in blood)
Inhibitors Tubule (PCT)

Loop Diuretics (aka High- Thick ascending loop (TAL) Inhibits Na-K-2Cl co-transporter •Electrolyte Imbalance (reduced levels)
ceiling diuretics) •Sulfa-related reactions (SJS, Hemolytic Anemia)
•Ototoxicity (ethacyrynic acid
•HyperGLU (Glycemia, Lipidemia, Uricemia)
Thiazide Diuretics Distal Convoluted Tubule Inhibits NaCl co-transporter •Electrolyte Imbalance (reduced levels)
(DCT) •Sulfa reactions
•HyperGLUC Glycemia, Lipidemia, Uricemia, Calcium)
K-Sparing Diuretics Collecting Duct Aldosterone Antagonism (S, E) •Hyperkalemia
Epithelial Na Channel Inhibitor •Spironolactone ( anti-androgen effects like gynecomastia)
(ENAC inhibitors) (A, T) •Triamterene: Increased risk of renal stone formation
Aquaretic (Mannitol) PCT, TAL (Loop of Henle) Creates an osmotic gradient in •Dehydration
H2O-permeable sites (PCT, TAL) •Hypovolemia
•HYPERnatremia (due to low blood volume)
DRUGS FOR CARDIOVASCULAR DISEASES : Hypertension

SYMPATHOPLEGICS

SYMPATHOPLEGICS

Centrally-Acting: Peripherally-Acting:
Ganglionic Blockers Alpha Blockers Beta Blockers
Alpha-2 Agonists Adrenergic Neuronal
Blockers

Hexamethonium -zosins -olols


Clonidine Exocytosis
Storage Inhibitor
Inhibitor

Reserpine Trimethaphan
Methyldopa
Guanethidine

Mecamylamine
Guanfacine
Guanedrel

Guanabenz
Bretyllium
DRUGS FOR CARDIOVASCULAR DISEASES: Hypertension

DIRECT VASODILATORS

MECHANISMS OF VASODILATION

Increased Nitric Potassium-Channel L-Type Ca Channel Endothelin Alpha-1


Blocker D1 Activation
Oxide Opening Antagonism Blockers

-dipines, Non- Fenoldopam Bosentan -zosins


Hydralazine DHPs
Minoxidil

Tezosentan
Na
Nitroprusside Diazoxide

DIRECT VASODILATORS

Pure Arteriolar Mixed L-Type Ca Channel


Vasodilators Vasodilators Blockers

Based on Chemistry Based on Duration •No RT and PE with LAL


•S/E: Hydralazine
Na Nitroprusside and Felodipine XR
Reflex Tachycardia (RT)
Peripheral Edema (PR)
•Remedy: Dihydropyridines Non-DHPs Short-Acting Long-Acting Modified
For RT: give Beta-blockers Minoxidil (LAL) Long -Acting
For PE: Give
-dipines Diltiazem •All Non-DHPs •Lercanidipi •Felodipine
Diuretics/ACEi/ARBs
•Majority of ne XR
Diazoxide DHPs EXCEPT •Amlodipine (originally
LAL •Lacidipine SA)
Verapamil
DRUGS FOR CARDIOVASCULAR DISEASES : Hypertension

ANGIOTENSIN ANTAGONISTS

SYMPATHOPLEGICS

Inhibits Synthesis of Inhibits Action of


Angiotensin II Angiotensin II

Direct Renin ACE Inhibitors ARBs


Inhibitor (-pril)

Aliskiren -sartan
Acute ACEi’s Rest are
(non-prodrug) Prodrugs

Captopril

Lisinopril

Enalaprilat
DRUGS FOR CARDIOVASCULAR DISEASES: Angina Pectoris

ANTI-ANGINALS

ANTI-ANGINALS

Calcium Channel
Nitrovasodilators Beta-Blockers
Blockers

Low Dose High Dose Non-DHPs Long-Acting DHPs Short-Acting DHPs

Sublingual Parenteral NOTE:


Verapamil Lercanidipine CONTRAINDICATED
unless used for
PRINZMETAL, but:
Very Short- Short-Acting Intermediate- Long-Acting Diltiazem Amlodipine
Acting Acting
Combine with
•Amyl Nitrate •Nitroglycerin •Nitroglycerin •Nitroglycerin Beta-Blockers, OR
(Inhalational) tablet (SL) tablet (PO) transdermal Lacidipine
•Isosorbide •Isosorbide patch Use Modified
Dinitrate Dinitrate •Isosorbide Release
tablet (SL) tablet (PO) Dinitrate SR preparation (i.e.
tablet (PO) Felodipine XR)
•Isosorbide
Mononitrrate
tablet (PO)

•Amyl Nitrate = Ax: CN Poisoning


•ISDN = adjunct for HF (given with HYDRALAZINE
for AFRICAN-AMERICAN PX)
DRUGS FOR CARDIOVASCULAR DISEASES: Heart Failure

Drugs for Heart Failure


Drugs for Heart Failure

Inotropic Agents Unloader Medications

Cardiac Endothelin
Beta-1 Agonists Bipyridines ACEIs/ARBs Diuretics Vasodilators Beta Blockers
Glycosides Antagonists
(PDE-3 inh)

Hydralazine
Digoxin Dobutamine Bosentan Bisoprolol
+ISDN
Inamrinone

Metoprolol
Digitoxin Dopamine Nesiritide Tezosentan
succinate
Milrinone

Carvedilol

Nebivolol
DRUGS FOR CARDIOVASCULAR DISEASES: Arrhythmia

Drugs for Heart Failure

ANTI-ARRHYTHMICS

Class I: Sodium Class II: Beta- Class III: Potassium Class IV: Calcium- Miscellaneous
Channel Blockers Blockers Channel Blockers Channel Blockers Agents
(Non-DHP)
Sotalol (only
Criterion IA IB IC Amiodarone Dronedarone Class III Beta- Miscellaneous Digoxin
+
blocker)
Na Blockade Moderate Weak Strong Diltiazem

Adenosine
Action Prolong Shorten No effect Bretyllium
Potential
Duration Verapamil Magnesium
Sulfate
Examples Disopyramide Tocainide Moricizine
Quinidine Mexiletine Flecainide Dofetilide
Procainamide Lidocaine Propafenone
Phenytoin Encainide

Ibutilide
DRUGS FOR GASTROINTESTINAL DISORDERS

DIARRHEA

Zinc Sulfate = for Kaopectate Colloidal Bile Salt- Octreotide


Oral Rehydration Probiotics Bismuth Opioids Atropine Racecadotril
children Binding Resins
Salts Compounds

Diphenoxylate Cholestyramine

Colestipol
Loperamide

Colesevelam
CONSTIPATION

Type of Laxative Example


Bulk-forming Psyllium, Methylcellulose, Polycarbophil

Stool Softener/Emollient Docusate sodium, Glycerin, Mineral oil

Osmotic MgO, Sorbitol, Lactulose, Magnesium citrate,


Sodium phosphate, PEG
Stimulant/Irritant Anthraquinone Glycosides (Senna, Aloe, etc. )
Castor oil, Bisacodyl, Phenolphthalein
Type 2 Chloride Channel Lubiprostone
Activator
Opioid Receptor Antagonist Methylnektrexone bromide, Alvimopan,

Saline Fleet enema, Mg, citrate, Na biphosphate


DRUGS FOR GASTROINTESTINAL DISORDERS

DRUGS FOR ACID-PEPTIC


DISEASES

Protein Pump Inhibitors M1 Blockers Antacids Mucosal Antibiotics


H2 Blockers
(PPI) (-prazole) Protectants

Systemic Non-Systemic Clarithromycin


Cimetidine Pirenzepine Sucralfate
Omeprazole
Sodium Aluminum
Bicarbonate Hydroxide Bismuth Amoxicillin
Esomeprazole Telenzepine Subsalicylate
Ranitine
Magnesium
Hydroxide Rebamipide Metronidazole
Lansoprazole
Famotidine
Alginate
Dexlansoprazole Tetracyclines

Nizatidine Misoprostol
Pantoprazole Nitroimidazole
Bismuth
Subsalicylate
Rabeprazole Potassium
DRUGS FOR GASTROINTESTINAL DISORDERS
DRUGS FOR IRRITABLE BOWEL DRUGS FOR INFLAMMATORY BOWEL SYNDROME
SYNDROME

5-HT3 Antagonist 5-HT4 Agonists Cl Channel Type of Drug Example


Anticholinergic Drugs
(IBS-Diarrhea) (IBS-Constipation) Activator Hydrocortiosne, Prednisone, Prednisolone, Methylprednisolone,
Corticosteroids
Dexamethasone
Cisapride Aminosalicylates Sulfsalazine, Mesalamine, Balsalazide, Olsalazine
Dicyclomine Alosetron Lubiprostone
(partial)
Immunosuppressants Azathioprine, 6-Mercaptopurine, Methotrexate, Cyclosporine,
Mycophenolate
Hyoscyamine Tegeserod Biologic Agents Infliximab, Adalimumab, Certolizumab
Cilansetron
(partial)
Anitibiotics Metronidazole, Ciprofloxacin, Rifaximin

Prucalopride Antidiarrheals Codeine, Diphenoxylate + Atropine, Loperamide, Cholestyramine


(full)
Monoclonal Antibodies Natalizumab

H2 Receptor Antagonists Cimetidiine, Ranitidine, Famotidine, Nizatidine


ANTI-EMETICS
Proton Pump Inhibitors Omeprazole, Lansoprazole, Esomeprazole, Rabeprazole, Pantoprazole

Anticholinergics Dicyclomine, Hyoscyamine


Type of Drug Example
Cholinomimetics Neostigmine, Bethanechol

D2 Receptor antagonists Metoclopramide, Domperidone

H1 Blockers Diphenhydramine, Phenothiazines, Orphenadrine

Antimuscarinics Scopolamine

Corticosteroids Dexamthasone

Cannabionoid Receptor Agonists Dronabinol, Nabilone

5-HT3 Receptor Antagonists -setrons


HORMONAL AGENTS
ESTROGEN-BASED DRUGS

Progesterone Selective Estrogen


Derivatives Estrogen Receptor Aromatase
GnRH Agonists Receptor
Downregulator Inhibitors
(Progestins) Modulators

Medroxyprogesterone
Acetate (Depo-provera) Gonadorelin Fulvestrant Tamoxifen Anastrozole

Norethindrone Goserelin Raloxifene (for Letrozole


osteoporosis)
Ethynodiol Diacetate Buserelin
Clomiphene/
Exemestane
Desogestrel Clomifene (for
Leuprolide infertility)
Dydrogesterone

Levonorgestrel
TESTOSTERONE-BASED
Megestrol
DRUGS CORTICOSTEROIDS
Norgestrel Androgen 5-alpha-
GnRH
Receptor reducatase
Antagonists
Norgestimate
Blockers Inhibitors

Prednisone Methylprednisolone
Flutamide Abarelix Finasteride
Progesterone

Bicalutamide Cetrorelix Dutasteride

Nilutamide Degarelix

Ganirelix
ANTI-CANCER AGENTS

Cytotoxic Agents

DIRECT DNA-Interacting agents

AlkylatingAgents
Agents Topoisomerase Inhibitors Antitumor Antibiotics
Alkylating
Dactinomycin
Mitomycin Bleomycin
Anthracyclines (Actinomycin D)
Mechlorethamine Camptothecins Podophyllotoxin
Derivatives
Cyclophosphamide
Irinotecan Doxorubicin
•Phospharamide Mustard
•Acrolein Etoposide

Topotecan Daunorubicin
Busulfan
Teniposide
Carmustine and Idarubicin
Lomustine

Altretamine Epirubicin

Procarbasine and
Dacarbazine
Mitoxantrone

Temsolomide

Cisplatin, Carboplatin,
and Oxaplatin
ANTI-CANCER AGENTS

Cytotoxic Agents

INDIRECT DNA-Interacting Agents

Folic Acid Antitumor Antibiotics


Antagonists

Pyrimidine Deoxycytidine Purine Taxanes Vinca Alkaloids Estramustine


Methotrexate Pemetrexed
Analogues Analogues Antagonists

6-Mercaptopurine Paclitaxel Docetaxel Cabazitaxel Vincristine


5-Fluorouracil Cytarabine

6-Thioguanine Abraxane Vinblastine


Capecitabine Gemcitabine
Fludarabine
Vinorelbine

Cladribine
ANTI-CANCER AGENTS

Targeted Therapy

TARGETED THERAPY

Anti- Anti-ALK BCR-ABL EGFR Tyrosine


Anti-EGFR mTOR B-Raf
VEGF/VEGFR Tyrosine Tyrosine PD-1 Blocker Ipilimumab Kinase Anti-CD20
Agents Inhibitors Inhibitor
Agents Kinase Agents Kinase Agents Inhibitors

Cetuximab Bevacizumab Alectinib Imatinib Pembrolizumab Erlotinib Everolimus Dabrafenib Rituximab

Panitumumab Ziv-aflibercept Nivoluman Gefitinib Temsirolimus

Regorafenib

Ramucirumab
•EGFR = Epidermal growth factor receptor
•VEGFR = Vascular Endothelial Growth Factor
Receptor
•ALK = Anaplastic Lymphoma Kinase
•BCR-ABL = Breakpoint Cluster Region – Abelson
•B-RAF = type of proto-oncogene
•mTOR = Mammalian target of rapamycin
•PD-1 = Programmed Cell Death Protein 1
•CD20 = Cluster of Differentiate 20
ADDITIONAL INFO
(No particular order)
SYMPATHETIC NS PARASYMPATHETIC NS

Biosynthesis •Metyrosine = inhibits RLS •Hemicholinium = inhibits RLS


Interfers with conversion of tyrosine  L-DOPA via Blocks the uptake of choline into the
inhibition of tyrosine hydroxylase presynaptic cell

Storage •Reserpine = inhibits vesicular uptake of NE Vesamicol = inhibits vesicular uptake of Ach

Exocytosis •Stimulates release of sympathetic •Stimulates release of Ach:


neurotransmitters: Alpha-Latrotoxin
Amphetamine •Inhibits release of Ach:
Ephedrine Botulinum Toxin
Tyramine
Angiotensin II
•Inhibits release of sympathetic neurotransmitters:
Guanethidine
Guanadrel
Bretylium

Metabolism •MAO •AChE


•COMT
HTN Emergency HTN Urgency
•Elevated BP •Elevated BP
•w/ End Organ Damage: •NO end organ damage
•Stroke
•Myocardial infarction
•Intracerebral
hemorrhage
•Eclampsia

Drug PG Type Effect Use

Misoprostol PGE-1 Cytoprotection •NSAID-induced ulcer


•Opening of Ductus Arteriosus

Epoprostenol PGI-2 Vasodilation •Primary Pulmonary HTN

Dinoprostone PGE-2 Cervical ripening •US-approved abortificacient

Alprostadil PGE-1 Vasodilation (in local •Erectile Dysfunction (male-assited


penile tissue) suppository)

Latanoprost PGF-2α Reduced intraocular •Glaucoma


pressure *Off-label: eyelash growth enhancer
SUMMARY OF DRUGS THAT ACT ON SEROTONIN RECEPTORS

Receptor Location Effect Drugs


5-HT1A CNS (pre-synaptic) ↓ release of 5HT (inhibitory effect) Buspirone (partial; anxiolytic)

5-HT1B/1D Cerebral blood Vessels cerebral vasoconstriction (anti- -triptans (migraine headache)
migraine effect)

5-HT2A/2B Smooth muscles contraction of smooth muscles Ergotamine (migraine headache)


•Oxytosis (uterine contraction; Ergonovine (post-partum bleeding)
opposite of tocolysis) Methysergide (prophylaxis of migraine)
•Bronchospasm Ketanserin (anti-HTN)
•Vasoconstriction

Platelets Platelet aggregation Ritanserin (inhibit platelet aggregation)


5-HT3 Chemoreceptor Trigger Zone Emesis -setrons (Chemotherapu-induced N&V)
*Alosetron ( IBS-diarrhea)

5-HT4 GI Tract Peristalsis Cisapride (partial)


Tegaserod (partial)
Prucalopride
^^ IBS-constipation
Partial Agonists Full Agonists Mild to Moderate Agonist Full ANTAGONISTS Relievers Controllers
(MORphine and (CODeine and Friends + Tramadol) Beta-2 Agonist: Beta-2 Agonist: Salmeterol, Formoterol
friends) Salbutamol/Albuterol
Terbutaline Muscarinic Antagonist:
•NalBUphine •Morphine •Codeine •Naloxone Tiotropium Bromide
•BUtorphanol •Apomorphine •Hydrocodone •Naltrexone Muscarinic Antagonist:
Methylxanthine:
•BUprinorphine •Hydromorphone, •Oxycodone •Nalorphine Ipratropium Bromide
Theophylline
•Pentazocine •Oxymorphone •Tramadol •Nalmethine
Methylxanthine: Mast Cell Stabilizers:
(partial Kappa •Methadone •Levallorphan Aminophylline Cromolyn Na
agonist) •Levorphanol Nedocromil
•Fentanyl
Leukotriene Modifiers
LOX inhibitors: Zileuton
LTD-4 receptor Antagonists: -lukast

Inhaled Corticosteroids
Budesonide
Type MOA Examples Fluticasone
Mucoregulators Increases H2O portion of bronchial Ambroxol Triamcinolone
gland  allows easier expectoration Bromhexine
Carbocisteine

Mucolytics Breaks down disulfide linkages NAC


between mucus molecules Levothyroxine (L-T4) Liothyronine (L-T3)

Antitussives Blocks peripheral cough receptors Codeine


Suppresses cough reflex center in the Dextromethophan → Most abundant → Most potent
brain Noscapine → For maintenance → For emergency (eg.
Butamirate Citrate (Sinecod)
=non-narcotic → Longer half-life Myxedema coma)
→ Shorter half-life
Expectorant Stimulates bronchial glands to secrete Guaifenesein
more H2O
Effort angina Prinzmetal angina Important Counseling Points for Bisphosphonates:
Aka Stable angina, Classic angina, Aka vasospastic angina, variant
Never take the drug at bedtime
typical angina angina, rest angina Always take the drug in an upright position, and remain in such
Effort-induced; precipitated by Not effort-induced; happens at position for at least 30 minutes after (to minimize irritation as they are
physical exertion rest known to cause esophageal irritation)
Drugs: Beta-blockers (reduces Drugs: Nitro vasodilators ( to Patient should take the drug on an EMPTY stomach with a full glass
inotropy and chronotropy), CCBs relax coronary artery) of water as oral absorption of these drugs decrease with intake of food
(Verapamil, Diltiazem, Long-acting
DHPs)

POISON ANTIDOTE
Acute Lead Poisoning (<24 Chronic Lead Poisoning Paracetamol N-acetyl-cysteine
hrs): (>3 mos): Atropine -stigmines
Encephalopathy Burton’s lines
Milky vomitus, Anemia Organophosphate 1st 24 -48 hrs: Atropine and Pralidoxime
Melena Developmental delay >48 hrs: Atropine
Wrist drop and foot drop
Warfarin Vitamin K

Heparin Protamine Sulfate

Opioid Naloxone
Pro-aggregants Anti-aggregants
Benzodiazepine Flumazenil
Platelet-derived Endothelial cell-derived
Stimulated: CLOTTING Stimulated: BLEEDING Digoxin Lidocaine IV (Digoxin-Induced Ventricular
Inhibited: BLEEDING Inhibited: CLOTTING Tachycardia)
Digifab or Digibind (Digoxin toxicity with no
Examples: Examples: arrhythmia)
•ADP •cAMP Phenytoin (Digoxin-induced Tachyarrhythmia)
•Serotonin •PGE
•TXA2 •PGI2 Beta blockers Glucagon
ANTIBIOTICS SPECTRUM OF ACTIVITY
AGENT EFFECT RESCUE DRUG
Cisplatin, Nephrotoxicity Amifostine,
Carboplatin hydration
Cyclophosphamide, Hemorrhagic cystitis (due MESNa
Ifosfamide to accumulation of
acrolein)
Doxorubcicin Caridotoxicity Dexrazoxane
Irinotecan, Diarrhea Hydration
Topotecan
Busulfan, Pulmonary fibrosis Supportive
Bleomycin treatment only

Methotrexate Hepatotoxicity Leucovorin,


Folinic Acid
Pharmaceutic Alternatives Same API, different dosage forms, salts, esters, or
complexes
Pharmaceutic Equivalents Same API and dosage forms but may differ in shape, LUNA = Lipophilic, Unionized, Nonpolar, ABSORBED
excipient, or scoring HIPE = Hydrophilic, Ionized, Polar, EXCRETED
Bioequivalent Pharmaceutical equivalents having similar rate and
extent of absorption
Therapeutic Equivalent Same safety and efficacy profile
Weak Acid Weak Base
Absorbed ACIDIC BASIC
Excreted BASIC ACIDIC

CLASS II CLASS I
PhenyBINGGE DilTheoMet ProParaVer
High Vd Low Vd
Phenytoin, Bicalutamide, Diltiazem, Theophylline,
PERMEABILITY

•Intracellular (well-deposited in •Extracellular


Ibuprofen, NSAID Metoprolol, Propranolol tissues) •Intravascular (in blood vessels)
• Extravascular •EXAMPLES
(aceclofenac), Griseofulvin, Paracetamol, Verapamil
•EXAMPLES:  Midazolam
Glibenclamide, Ezetimibe Atropine Warfarin
Beta blockers
CLASS IV CLASS III  Chloroquine
NeoCCAARE
𝑉𝑑 = 𝐷𝑜𝑠𝑒
Furosemide, HCTZ, Neomycin, Cimetidine, Captopril, 𝑃𝑙𝑎𝑠𝑚𝑎 𝑐𝑜𝑛𝑐𝑒𝑛𝑡𝑟𝑎𝑡𝑖𝑜𝑛 (𝐶)
Captopril, Bifonazole, Atenolol, Acyclovir, Ranitidine, •Vd is directly proportional to dose of the drug
Enalapril •Vd is indirectly proportional to the drug plasma concentration
Cefuroxime •Thus, high plasma concentration results in a decrease in Vd

SOLUBILITY
Zero Order Kinetics First Order Kinetics
Phase I : Functionalization Phase Phase II : Conjugation Phase
→ Amount is fixed → Amount is not fixed
→ Rate is fixed → Rate is not fixed Unmasking polar functional group → Addition of polar functional group
→ Independent on concentration → Dependent on concentration
(not proportional (proportional)
•Oxidation •Glucuronidation
→ Elimination for certain drugs : → Elimination for majority of drugs •Reduction •Amino acid conjugation
Zero WHATTS Power •Hydrolysis •Glutathione conjugation
•Warfarin •Sulfation
•Heparin •Acetylation
•Aspirin, Alcohol •Methylation
•Theophylline
•Tolbutamide
•Salicylates
•Phenytoin

Glomerular Filtration Rate  Inulin, Creatinine


Active Tubular Secretion  p-aminohippuric acid, Iodopyracet
Extracellular Fluid 🡪 Inulin, Thiosulfate, Mannitol, Bromine
Plasma Volume 🡪 Evans blue, Tryptan red

You might also like