Pharmacology Scheme

3rd professional
By: Hafiz Muhammad Attaullah &
Aqib Razzaq
(Session 2016-21)

For any correction and

suggestion mail at

attaullah@inbox.eu
aqib6razzaq@gmail.com

AttaUllah
attaullah@inbox.eu

Drug classification
Benzodiazepines: are widely used anxiolytics, barbiturates are relpaced by benzodiazepens due to their greater adverse effects(have no GABA mimetic action)
Benzodiazepines
Short acting(3-8 hrs)
Triazolam, midazolam, oxazepam
Intermediate acting(10-20 hrs)
Alprazolam, temazepam, lorazepam
Long acting(1-3 days)
Diazepam, flurazepam,
clorazepam, lorazepam
[Flumazenil(antidot of BZ,GABA
antagonist, i.v,short H.L,)]
Barbiturates: these agents are formely used to sedate the patients and induce sleep, now they are replaced by BZ, due to their more adverse effects,
tolerence and depensence.( have GABA mimetic action)
Barbiturates
Ultra short acting(20-30 min)
Thiopental, methohexitone
Short acting(3-8 hrs)
Phentobarbital,secobarbital,
amobarbital
Long acting(1-2 days)
Barbital, phenobarbital
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Chp-1 DRUGS ACTING ON CENTRAL NERVOUS SYSTEM
a) SEDATIVE & HYPNOTICS, ANXIOLYTICS
Mechanism of action pharmacokinetics Therapeutic use Adverse effects
Bind with GABA receptor at alpha &
gamma interface All anxiety disorders Drowsiness,
Well absorb orally, distributed in all
confusion, ataxia,
body tissues(CSF, CNS), met by
cognitive problems,
liver(CYP450), active metabolites,
insomnia(early
excreted in urine
morning), day time
Dependence:
anxiety, amnesia
psychological & physical
C.I in liver disease,
dependence(if prolonged used),
acute angle
with drawl symptoms(more with
glaucoma, with
short acting not with long acting)
alcohol(↑effect),
cross tolerance may occur
pregnancy
Prolong the duration of GABA(↑ Cl- )
Block excitatory glutamate receptors,
at high conc. Block Na+ channels)
Well absorb orally, distributed in all
body tissues(CSF, CNS), met by
liver(CYP450), inactive metabolites, Same as above but
Same as above
excreted in urine more adverse effects
Dependence: same as above but
more
1

Non benzodiazepine
hypnotics
Zolpidem, zopiclone, Zaleplon(1
hrs half life, best)
Melatonin receptor agonist
Ramelteon
Antidepressants ( doxepin) see
next for detail
Antihistamines(hydroxyzine,
diphenhydramine)
Depression: is a state of mind, symptoms include sadness, hopelessness, inability to feel pleasure, disturbance in sleep patterns, loss
of energy and suicidal thoughts.
Selective serotonin reuptake inhibitors( SSRIs): selectively inhibit serotonin reuptake, 300-3000times more selective towards serotonin transport, better than others i.e
SNRIs
Selective serotonin reuptake
inhibitors( SSRIs)
Fluoxitine, fluvoxamine
Citalopram, escitalopram,
Serotonin-norepinehrine reuptake inhibitors( SNRIs): used when SSRIs are ineffective
Serotonin-norepinehrine
reuptake inhibitors( SNRIs)
Venlafaxine, desvenlafaxine,
duloxitine, levomilnacipran
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Bind with benzodiazepines subtype BZ1
Agonist of MT1 & MT2
Melatonin is a hormone, secreted
from pineal gland during sleep,
maintain cardiac rhythm and normal
sleep cycle.
b) Antidepressants
Block reuptake of serotonin
↑ neurotransmitter in synaptic cleft
↑neuronal conduction across the
synaptic cleft.
Block reuptake of serotonin and
norepinephrine
↑ neurotransmitters in synaptic cleft
↑neuronal conduction across the
synaptic cleft.
Well absorb orally, distributed in all Same as above
body tissues(CSF, CNS), met by But no anticonvulsant effect
liver(CYP450), active metabolites, No muscle relaxing property
excreted in urine Major use in insomnia
Well absorb orally, distributed in all
body tissues(CSF, CNS), met by
Insomnia
liver(CYP450), active metabolites,
excreted in urine
Depression, psychatric disorder,
Well absorb orally, distributed in all
obsessive compulsive disorder,
body tissues (CSF, CNS), met. by panic disorder, GAD, post
liver (CYP450 , CYP1A2 ,CYP3A4) traumatic stress disorder,
excreted in urine premenstural dysphoratic
disorder
Depression, chronic painful
disorder, backache, muscle
Same as above
ache, diabetic neuropathy,
neuralgia, fibromyalgia
2
Less than
benzodiazepines
Night mares,
agitation,
anterograde amnesia,
headache, G.I upset,
dizziness, day time
drowsiness
Dizziness, fatigue,
somnolence(excessive
sleep), ↑ prolactin
level
Sleep disturbance, fever
in children, suicidal
thoughts, sexual
dysfunction, nausea,
anxiety, drowsiness
Discontinuous
syndrome(flu-like
symptoms, malasia,
headache, agitation)
Nausea, headache,
sexual dysfunction,
dizziness, insomnia,
constipation,
somnolence.
Discontinuous
syndrome
Norepinephrine-dopamine reuptake inhibitors( NDRIs): mostly classified as atypical antidepressents
Norepinephrine-dopamine
reuptake inhibitors( NDRIs)
Bupropion
Atypical antidepressants: mixed group of agents has action on several differnet sites.
Atypical antidepressants
Mirtazepine
Nafazodone, trazodone,
vilazodone
Monoamine oxidase: is mitochondrial enzyme (in nerves, gut, liver), cause oxidative deamination of serotonin, norepinephrine and dopamine.
Monoamine oxidase inhibitors
Non selective
Phenelzine, isocarboxazid
Selective for MAO-A
Moclobemide
Selective for MAO-B
Selegiline, Resegiline
Tricyclic antidepressants
Tertiary amines: imipramine
Amitriptyline, clomipramine,
trimipramine, doxepin,
Secondary amines:
nortriptyline, protriptyline,
Tetracyclic:
maprotiline,amoxapine
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Weak Blocker of reuptake of
Norepinephrine and dopamine
↑ neurotransmitter in synaptic cleft
↑neuronal conduction across the
synaptic cleft.
Mirtazepine
Block presynaptic α2 receptors,
↑ release of serotonin and
norepinephrine, also block H1(histamine)
receptors
Nafazodone, trazodone
Weak inhibitor of serotonin reuptake,
block H1 receptors, block 5HTa2 receptors
on postsynaptic membrane, ↑neuronal
conduction across the synaptic cleft.
Drug inhibit MAO, ↓ degradation of
neurotransmitters (irreversibly e.g
phenelzine or reversibly)
Act by two ways.
1- Inhibition of N.T reuptake
2- Blocking of receptors
Block reuptake of serotonin and
norepinephrine similar to SNRIs,
Also block H1, muscarinic, α-receptors,
Amoxapine also block dopamine
receptors
doxepin, maprotiline( seletive reuptake
inhibitor of norepinephrine)
Well absorb orally, distributed in all Depression, Dry mouth, sweating,
body tissues(CSF, CNS), met by For with drawl symptoms of nervousness, tremors,
liver(CYP2D6), excreted in urine smoking seizures
Depression, insomnia Increase appetite,
weight gain, sedating
Well absorb orally, distributed in all
body tissues(CSF, CNS), met by
liver(CYP2D6), excreted in urine More sedating,
Depression, insomnia
hepatotoxic,
On-off disorder
orthostasis, dizziness
Drug food interaction(
Tyramine poisoning)
Well absorb orally, distributed in all Atypical depression, last agent
headache,
body tissues, met. by liver ,excreted for treatment
tachycardia, nausea,
in urine
hypertension,
seizures, stroke
Weight gain, dry mouth,
constipation, urinary
retention, blurred
Same as above
Moderate to severe vision, tachycardia,
Drug interactions:
depression, panic disorder arrhythmia, nausea,
TCAs+ MAOIs= mutual drowsiness, angle
Amitriptyline(in migraine),
enhancements of effect e.g ↑B.P, closure glaucoma,
imipramine( in bed wetting)
↑ Temperature orthostatic hypotension,
Dependence: discontinuous
TCAs+ ethanol or CNS depressants= sedation, dizziness,
syndrome
toxic sedation sexual dysfunction, may
↑ benign prostate
hyperplasia, epilepsy,
pre-existing arrhythmia
3
 Antimanic drugs (mood stabilizers)
Mania: is a bipolar disorder, characterize by elevated mood with feeling of excitement, ↓ sleep, ↑activity, sefl confidence
Lithium salts Headache, dry mouth,
Many cellular process alter but Absorb orally, well distributed,met
polydipsia,
mechanism is unknown, suppresses by kidney,can be used in liver No effect on normal person
polyphagia, polyuria,
patients excreted in urine, saliva, Used in Mania and hypomania
IP3 and DAG signaling, also ↓ G.I upset, fine hand
low therapeutic index, 20hrs half C.I: in pregnancy
hormone- induced cAMP tremors, dizziness,
life
production fatigue, skin reaction
Lithium salts Benzodiazepines
Lithium carbonate As previous As previous As previous
↑ GABA activity
Benzodiazepines Anticonvulsants
Anticonvulsants Carbamazepine(block Na+ channel,
Carbamazepine, valproic acid, inhibit nerve impulse generation),
lamotrigine valproic acid(block Na+ channel,
Atypical antipsychotics block T-type Ca+2 channel, block
Olanzapine, risperidone, clozapine GABA transaminase )
See next See next See next
Lamotrigine(block Na+ channel, block
voltage dependent Ca+2 channels)
Atypical antipsychotics
block dopamine receptors, block 5HT
particularly 5HT2a , muscarinic
blockage, adrenergic blockage
c) ANTIEPILECTICS
Epilepsy: it is not a single entity, it is chronic disease characterize by proximal brain dysfunction due to excessive neuronal discharge, associated with some alteration of
abnormal movement, atypical or odd Behaviour, distorted perception. About 10% people have no identified cause.
Well absorb orally,
Classification On the basis of types
distributed in body
of epilepsy Phenytoin
(CNS), phenytoin anf
Partial seizures block voltage gated Na+ channel
fosphenytoin bind
Simple Carbamazepine
with protein, other
Phenytoin, carbamazepine, block Na+ channel
less bounded, met by
lamotrigine lamotrigine
liver and kideny some
Complex block Na+ channels, and block high
by hydrolysis,
Phenytoin, carbamazepine, voltage gated Ca+2 channels
excretde in urine
lamotrigine
All have drug
Topiramate interactions(mostly
Generalized seizures + enzyme inducer)
Block voltage gated Na channels,
Tonic-clonic +2 Adverse effects
Block L-type Ca channels, carbonic
4
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Phenytoin,fosphenytoin anhydrase inhibitor, also act on Phenytoin
carbamazapine, lamotrigine, glutamate site CNS depression,
topiramate Ethosuximide nystagmus, ataxia,
Absence Block T-type Ca+2 channels gingival hyperplasia,
neuropathy,
Ethosuximide, lamotrigine Valproic acid
osteoporosis
Myoclonic block Na+ channel, block T-type Ca+2 Carbamazepine
Valproic acid channel, block GABA transaminase Hyponatremia, not
Febrile uses given in absence
phenobarbital Phenytoin seizures
Status epilepticuc Focal and generalized seizures, status Lamotrigine
Phenytoin+ diazepam epilepticus Skin rashes, serious life
Other drugs Carbamazepine threatening disorders
Gabapentin,pregabalin, tiagabine, Tonic-clonic seizueres, trigeminal Valproic acid
zonisamide nuralgia, bipolar disorder Hepatotoxic in excess,
lamotrigine teratogenic
Focal and generalized seizures, bipolar
disorder

d) ANTIPARKINSONIANS AND OTHER NEURODEGENERATIVE DISEASES

Antiparkinsonians
Parkinsonism: it is progressive neurological disorder of muscle movement characterize by tremors, muscle rigidity, bradykinesia, postural and gait
abnormalities. Etiology- it is due to damage of substantia nigra results in destruction of nerve terminals to secrete dopamine in neostriatum

Levodapa+carbidopa
Dopamine receptor agonists
Bromocriptine(ergot derivative),
apomorphine, pramipexole, Uses. Parkinsonism,
ropinirole, rotigotine COMT-inhibitor wearing off
Monoamine oxidase Levodapa(cannot cross BBB) Well absorb orally, bound to albumin, limited
Precursor of dopamine, restore dopamine level phenomenon
inhibitor (type-B) distribution, met. By liver & kidney, excreted in urine
Selegiline, rasagiline Carbidopa and feces.
Anticholinergics Dopamine decarboxylase inhibitors MAOIs(met by liver, excreted In urine) Adverse effects
Benztropine, procyclidine, Dopamine receptor agonists Levodapa(rapid absorption by S.I, short half life, COMT-inhibitor
biperidine ↑ dopamine effect similar to levodopa others as above) Diarrhea, postural
Catechol-o-methyl transferase Monoamine oxidase inhibitor –type-B
hypotension,
inhibitors(COMT-inhibitor) Selectively inhibit Monoamine oxidase-B,↑ brain anorexia, dyskinesia,
Entacapone, tolcapone dopamine sleep disorder,
Amantadine(antiviral) Anticholinergics hallucinations
MAOIs.

5
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Block cholinergic transmission, produce effect Hypertension crisis
similar to increased dopamine, help to correct (Tyramine poisoning),
imbalance between dapamine and acetylcholine insomnia
COMT-inhibitor Levodapa
Reversibly inhibit COMT, ↓plasma conc. Of 3-o- PNS effects(G.I
methyldopa,↑ central uptake of levodapa,↑ brain upset,anorexia,
dopamine hypotension,
Amantadine ventricular
↑ release of dopamine, block cholinergic receptors, extrasystole,
block NMDA-type glutamate receptors +coomb’s teat) CNS
effects(dyskinesia,
sleep disorder,
hallucinations)

Anti-Alzheimer’s drugs
Dementia of Alzheimer type has three distinguish features. 1- accumulation of senile plaques. 2- formation of numerous neurofibrillary. 3- loss of cortical
neurons (cholinergic neurons). Drugs use to improve cholinergic transmission or to prevent excitotoxic action of overstimulation of NMDA-glutamate
receptors in brain.

Reversible acetylcholine esterase Acetylcholine esterase inhibitors G.I upset, tremors,

inhibitors
Galantamine
Irreversible acetylcholine
esterase inhibitors
Donepezil, tacrine
Rivastigmine (for dementia),
NMDA-receptor antagonist
Memantine
inhibit acetylcholine esterase ,
↑ cholinergic transmission
NMDA-receptor antagonist
Block NMDA-type glutamate
receptors, inhibit glutamate
transmission, ↓ influx of Ca+2
Well absorb orally, distributed in
body tissues, met by liver, excreted
in urine
bradycardia, muscle
cramps, anorexia
Alzheimer’s disease,
Helps in improvement of
cognition Dizziness, confusion,
agitation, restlessness

6
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 e) ANTIPSYCHOTICS (also called neuroleptics or tranquilizers)
Primarily used to treat schizophrenia, often used in combination, also effective in other psychotic disorders and manic states
Extrapyramidal
symptoms,
Typical (1st generation drugs)
↑ cholinergic action,
Typical (1st generation drugs) Competitive inhibitors at variety of
Oral absorption is variable, large dystonia, akathisias,
High potency receptors, block dopamine
volume of distribution, passes in Reduce symptoms of rigidity, tremors,
Haloperidol, fluphenazine, receptors(D2)
brain, met. by liver CYP450, schizophrenia, prevent from neuroleptics,
pimozide, thiothixene,
excreted in urine nausea, vomiting, can be used malignant syndrome
Prochlorparazine
2-4 weeks effects as tranquilizers, hiccups, Cholinergic
Low potency
Atypical (2nd generation drugs) C.I phonetics of Tourette blockage(urinary
thioridazine, chlorpromazine
block dopamine receptors (D2) in Seizures, cause mood change, disorder, autism, for retention, weight
Atypical (2nd generation drugs) suicidal thoughts, alcohol with refractory depression
brain and periphery, block 5HT2a , gain, seizures,
Quetipaine, risperidone,
little blockage on muscarinic, drawl patients sedation, postural
olanzapine, clozapine, aripiprazole
α-adrenergic and histaminergic hypotension, dry
receptors mouth, sexual
dysfunction)
f) OPIOID ANALGESICS
Opioids are natural, semi-synthetic and synthetic compounds that produce morphine like effects, all opioids act by binding to Three receptor families, designated as μ(mu),
ẟ(delta) and ҡ(kappa)
A.E: GI disturbance,
hypotension,
OPIOID AGONISTS Morphine: Morphine and other
Actions: MARPHINE CVS* constipation,
Strong Agonists analgesics exert their effect by
Orally absorb very slow, Miosis, Analgesia, Respiratory confusion, headache,
Morphine, Remifentanil, interacting stereospecifically with
Administered as IV, IM, S.C. depression, Physical and acute morphine
Sufentanil, Alfentanil, Fentanyl Opioid receptor on membrane of
Metabolize in liver by glucuronoids Psychological dependence, poisoning, skin
Heroin, Methadone, Oxycodone certain cells in CNS, and other
conjugation, Histamine release, rashes, Addiction,
Moderate Agonist anatomic structure, GI tract and the
Morphine 6-glucuronoids its Hypotension, Hypothermia, dysphoria, drug
Codeine Urinary bladder. Morphine act at ҡ
metabolite is more potent. Itching, Nausea & vomiting, dependence,
Partial Agonist receptor in lamina 1 & 2 of dorsal
Extensive first pass metabolism. Euphoria, Constipation, Vegal respiratory
Buprinorphine horn of spinal cord, ↓release of
Enter all body tissue, stimulation ,Sedation and depression etc.
Weak Agonist substance P which modulate pain
widely distributed in body, hypnosis. Drug interaction:
Propoxyphene receptor. Also inhibit the release of
Cross placenta, orally small amount C.I: Head injury, Asthma, Depressant action
( Structural analogue of many excitatory transmitters from
cross BBB. COPD, Infants, pregnancy, enhanced by
Methadone) nerve terminal which carrying
hypotension. phenothiazines,
nociceptive (painful) stimuli.
MAOIs and tricyclic
antidepressants.

7
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Fentanyl: Synthetic Opioid chemically
related to morphine, 100 times more
analgesic potency then morphine.
Remifentanil, Sufentanil, Alfentanil:
Similar to Fentanyl. Sufentanil more
potent the Fentanyl. Used as
anesthesia.
Methadone: Action mediated by μ
receptor and also antagonist of
NMDA and norepinephrine and
serotonin reuptake inhibitor.
Codeine: less potent then morphine,
Analgesic action of codeine are
derived from its conversion to
morphine by the CYP450 2D6
enzyme system
Buprinorphine : Act at μ receptor
similar to morphine
Major use Opioid detoxification.
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Given IV and transdermal, epidural, Similar to morphine but less A.E: Similar to
intrathecally, Highly lipid soluble, except analgesia, Few morphine.
Metabolize by CYP 450 cardiovascular effects, Used as C.I: Head injury,
3A4.Eliminated in urine. analgesic to supplement Asthma, COPD,
Short duration of action (5-30 anesthetic, cancer pain, Infants, pregnancy,
minutes),analgesic eff. In 5 min. postoperative pain, in labor. hypotension.
Orally well absorbed, IM Actions similar to morphine A.E: Similar to
Biotransformed in liver, met. by butt slowly. morphine.
CYP450 isoenzyme,excreted in Use in treatment of both C.I: Head injury,
feces. Very lipophillic and nociceptive and neuropathic Asthma, COPD,
accumulated in fat tissues. pain. Also used as substitution Infants, pregnancy,
Long duration. therapy in Opioid dependence hypotension.
A.E: Main side effect
is Constipation and
For mild to moderate pain,
sedation,
Used in combination with
Administered orally, Convulsions,
acetaminophen for
Metabolized by liver hallucinations
management of pain, good
Excreted in urine. GI disturbance.
antitussive activity used in
C.I: Asthma,
coughs preparations.
Respiratory
depression.
A.E: Similar to
Similar to morphine, more potent morphine but less
IM, IV sublingual analgesic than morphine, Less marked, Constipation
Very lipophillic tolerance, dependence: Use in less marked, Postural
Long duration of action post operative pain, cancer pain, hypotension
Metabolized by liver preanesthatic, Also used as prominent,
Excreted in bile and urine substitution therapy in Opioid Its action is not
dependent subjects. complete reversed by
Naloxone.
8

Pentazocine: It has agonist action at
MIXED AGONIST ANTAGONIST Ҡ-receptor and weak antagonist
Pentazocine action at μ & ẟ-receptor. Promote
Nalbuphine analgesia by activating receptors In
the spinal cord.
Tramadol: Synthetic codeine
derivative and a centrally acting
OTHER ANALGESICS
analgesic bind to the μ Opioid
Tramadol
receptor.
Tapentadol
Also inhibit reuptake of
Norepinephrine and 5-HT.
Naloxone: A competitive antagonist
at μ, ҡ and ẟ receptor with a 10-fold
higher affinity for μ then for ҡ
receptor.
OPIOID ANTAGONISTS(antidot)
Naloxone
Naltrexone
Naltrexone similar to Naloxone but
more potent and long duration.
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Orally, IM,SC
May be metabolize in liver
And may be excreted in urine.
Orally, IM, IV
Metabolize in liver. Extensive
metabolize via CYP450 2D6 leading
to active metabolize which is more
active.
Excreted may be in urine
No effect orally due to high first
pass metabolism,
Administered IV.
Given in combination with Opioids.
Naltrexone orally used in
combination with clonidine for
rapid Opioid detoxification
9
A.E: less euphoria
then morphine,
Similar to morphine but less.
dysphoria,
Used in traumatic and
tachycardia,
postoperative pain.
nightmares,
At high dose sympathetic
hallucinations ,
stimulation.
dizziness
C.I: In Angina patient.
A.E: Similar to
morphine
Similar to morphine but less. Drug interaction:
In mild to moderate pain due with SSRIs, MAOIs
to trauma and surgery or and tricyclic
cancer Naloxone can only antidepressant leads
partially reverse its effect. to toxicity manifested
by CNS excitation and
seizures.
Reverse the coma and
A.E: Nausea, vomiting
respiratory depression of
hypertension
Opioid overdose with 30sec
Pulmonary edema
after IV injection.Reverse the
Skin Rashes
effect of morphine overdose.
A.E: Headache,
tiredness, skin rashes,
Naltrexone sometime for
vomiting, Naltrexone
treating chronic alcoholism by
can leads to
unknown mechanism
hepatotoxicity.
C.I: In liver disease.

Oxygen (O2)
Introduction: It is a colourless,
tasteless and odorless gas. Oxygen is
essential for life.
Hypoxia: It is a life threatening
condition in which oxygen is
inadequate to meet the metabolic
demands of the tissue.
Oxygen Inhalation: oxygen inhalation
is used primarily to reverse or prevent
the development of hypoxia; other
consequences usually are minor.
Administration: Oxygen is supplied as
compressed gas in steel cylinder and
a purity of 99% is referred to as a
medical grade. Most hospitals have a
oxygen piped from insulated liquid
oxygen containers to areas of
frequent use.
Therapeutic uses: It is used for
correction of hypoxia, also for
reduction of partial pressure of inert
gas. As hyperbaric oxygen therapy in
treatment of trauma, bums, radiation
damage, infections and other
neurological condition.
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
g) THERAPEUTIC GASES
(Oxygen, Carbon dioxide, Nitric Oxide, Helium)
Carbon dioxide (CO2)
Introduction: CO2 is a colourless and
odorless gas and not supports
combustion.
Production & storage: Carbon dioxide is
produced by metabolism at
approximately the same rate as O2 is
consumed. CO2 diffuses readily from the
cells into the blood, where it is carried
partly as bicarbonate ion. CO2 is marked
in grey metal cylinder as pure gas or as in
combination with oxygen.
Administration: It is usually administered
as a concentration of 5-10% in
combination of O2by means of a face
mask. Another method
For temporary administration of CO2 is
rebreathing such as from an anesthesia
breathing circuit.
Therapeutic Uses: Used for insufflations
during endoscopic procedure, use to
flood the surgical field during cardiac
surgery, detoxification of heroin addict.
10
Nitric Oxide (NO)
Introduction: NO is a free radical gas
long known as an air pollutant and
potential toxin. NO in now known as a
critical endogenous cell signaling
molecule with an increasing number of
potential therapeutic applications.
Production & synthesis: Endogenous
NO is produced from L-arginine by a
family of enzymes called NO synthases
(neural, inducible and endothelial). NO
causes vasodilatation when synthesized
in response to shear stress, also inhibit
platelet aggregation and adhesion.
Inactivation: NO is rapidly inactivated
in the circulation by oxyheamoglobin
and by the reaction of NO with heme
iron and excreted in urine.
Therapeutic uses: When inhaled
selectively dilates the pulmonary
vasculature, for improvement of
oxygenation as in ventilation
Helium (He)
Introduction: Helium is an inert
gas whose low density, low
solubility and high thermal
conductivity provide the basic for
its medical and diagnostic uses.
Production & storage: Helium is
produced by separation from
liquefied natural gas and is
supplied in brown cylinder.
Administration: Helium can be
mixed with oxygen and
administered by mask or
endotracheal tube.
Therapeutic uses: The primary
uses of helium are in pulmonary
function testing, treatment of
respiratory obstruction, laser
airway surgery, determination of
residual lungs volume, functional
residual capacity.
 h) CNS stimulants, medullary stimulants, spinal cord stimulants
CNS effects(insomnia,
dizziness, tremors,
confusion, delirium,
Attention deficit hyperactive
panic states, suicidal
Amphetamine disorder(ADHD),
Amphetamine thoughts) CVS
↑ neurotransmission is synaptic narcolepsy(sleepy bouts in day effects(hypertension,
Smoked or I.V by abusers,
cleft, ↑release of intracellular Orally completely absorb, distributed in time), appetite supression palpitation, arrhythmia,
body(CNS), met by liver, excreted in urine C.I in cardiac patients, angina pain, circulatory
catecholamine, inhibit MAO, weak
hypertension, hyperthyroidism, collapse), G.I
reuptake inhibitor
Psychomotor stimulants glaucoma and history of drug effects(anorexia,
Amphetamine abuse nausea, vomiting,
Methyl phenidate, diarrhea)
dextroamphetamine
Xanthine derivatives Xanthine derivatives Xanthine derivatives :Orally
Methylxanthine, caffine, Muscle relaxants(asthma), 11affeine causes
↑translocation of extracellular Ca+2, completely absorb, distributed in
theophylline, theobromine used with insomnia, anxiety,
↑cAMP, ↑cGMP(caused by body(CNS, brain),cross placenta,
Nicotine analgesics(headache) in OTC agitation, at high dose
inhibition of phosphodiesterase, met by liver (CYP1A2), excreted in
cocaine drugs emesis convulsions
block adenosine receptors urine, milk
Psychotomimetic
drugs(hallucinogens)
Phencyclidine, Irritability, tremors,
Nicotine: Highly lipid soluble,
tetrahydrocannabinol, lysergic intestinal cramps,
readily absorb orally (G.I mucosa),
acid diethylamide Nicotine diarrhea, ↑ heart
lungs and skin, distributed in body Not currently used in
Ganglion stimulant by depolarization rate, enzyme inducer
(CNS, brain), cross placenta, (1-2 mg therapeutically
at high doses block ganglion With drawl
in cigarette) met. By lungs and
Dependence symptoms are
liver. Excreted in urine
Physical dependence develop common
rapidly, tolerance, drug seeking
behavior, with drawl
symptoms, Euphoria, tachycardia,
Cocaine Cocaine ↓respiration,
Block reuptake of monoamines in Minimum absorption by orally, agitation,
presynaptic terminals, ↑effects on powder is snorted, or Temporarily relieves severe hypertension,
monoamines in CNS and injected,(smoking is effective depression dyspnea, seizures,
periphery(dopamine pleasure route)met in liver, excreted in arrhythmias,
system) urine, milk respiratory failure,
death (Rip)

11
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 i) ANESTHETICS: GENERAL & LOCAL
Provides analgesic, amnesic, and unconscious, and provides muscle relaxation and suppression of undesirable reflexes.
Recovery: Recovery
is the time from
discontinuation of
Maintenance: Maintenance
Induction: It is period of time from administration of the
Preanesthetic medication: provides a sustained surgical
the onset of administration of the anes-thesia until
Antacid STAGES OF ANESTHESIA anesthesia. After adminis-
anesthetic to the development of consciousness and
Anticholinergics (Three stages) tering the selected anesthetic
effective surgical anesthesia in the protective physiologic
Antiemetics Induction mixture, the anesthesiologist
patient. Induction of anesthesia reflexes are regained.
Antihistamines Maintenance monitors the patient’s vital
depends on how fast effective Recovery is the reverse
Benzodiazepines Recovery signs and response to
concentrations of the anesthetic of induction and
opioids various stimuli throughout
drug reach the brain. depends on how fast
the surgical procedure
the anesthetic drug
diffuses from the
brain.
Stage IV (Medullary
Paralysis):
Stage III (Surgical Anesthesia):
Severe depression of
DEPTH OF ANESTHESIA Stage I (Analgesia): Loss of pain Regular respiration and
Stage II (Excitement): The patient the respiratory and
(Four sequential stage) sensation results from interference relaxation of the skeletal
experiences delirium and possibly vasomotor centers
Stage I (Analgesia) with sensory transmission in the muscles occur in this stage.
violent, combative behavior. occurs during this
Stage II (Excitement) spinothalamic tract. The patient is Eye reflexes decrease
There is a rise and irregularity in stage.
Stage III (Surgical Anesthesia) conscious and conversational. progressively, until the eye
blood pressure. Death can rapidly
Stage IV (Medullary Paralysis) Amnesia and a reduced awareness of movements cease and the
The respiratory rate may increase occur unless
pain occur as Stage II is approached. pupil is fixed. Surgery may
measures are taken to
proceed during this stage.
maintain circulation
and respiration.
General Anesthetics: Inhaled
(For the maintenance of anesthesia after administration of an intravenous agent)
General anesthesia is a reversible state of CNS depression, causing loss of response and perception of stimuli. Aims of anesthesia are sedation and reduction of anxiety,
lack of awareness and amnesia, skeletal muscle relaxation, suppression of undesirable reflexes and analgesia.
Volatile liquids Halothane: It is prototype drug of A.E: Bradycardia.
Oxidatively metabolized in the body Potent anesthetic but a
Halothane this group. No specific receptor. Cardiac arrhythmias.
to tissue-toxic hydrocarbons. relatively weak analgesic.
Halothane derivatives Increase the sensitivity of (GABAA) Concentration-
Accumulation of bromide and Co-administered with nitrous
Sevoflurane(choice for children) receptors to the inhibitory dependent
other toxic agents causes fever, oxide, Opioids, or local
Isoflurane(cheap) neurotransmitter, GABA. hypotension
followed by anorexia, nausea, and anesthetics.
Desflurane Postsynaptic neuronal excitability is Hepatitis
vomiting, and patients may exhibit Relaxes both skeletal and
Gas thus CNS activity diminished. The Some risk
signs of hepatitis. uterine muscle, also used in
Nitrous oxide activity of the inhibitory glycine hepatotoxicity
12
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)

Barbiturates:
Thiopental is a potent anesthetic
but a weak analgesic. It is an ultra-
short-acting and administered IV.
Quickly enter the CNS and depress
function.
Metabolized by the liver.
Thiopental has minor effects on
the cardiovascular system.
A.E: Apnea, coughing, chest wall
spasm and bronchospasm
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
receptors in the spinal motor
neurons is increased. Block the
excitatory postsynaptic current of the
nicotinic receptors.
Nitrous Oxide: “Laughing gas.
Not act on GABA. Mediated inhibition
of NMDA receptor .( glutamate main
excitatory neurotransmitter of body)
General Anesthetics: Intravenous
(Used for Rapid induction of anesthesia)
Benzodiazepines: Midazolam,
diazepam, lorazepam
Enhancing inhibitory effect of various
neurotransmitters like GABA and
minimal CV depressant
Used in combination with anesthetics
to sedate the patient. All three
facilitate amnesia while causing
sedation.
A.E: Ataxia, drowsiness, confusion,
amnesia.
13
obstetrics when uterine
relaxation is indicated.
Due to pleasant odor suitable
in children for inhalation
induction.
Alone no effect used in
combination with oxygen and
Poorly soluble in blood and other
other potent agent.
tissues.
Potent analgesic.
Move rapidly in and out of the body
Muscle relaxation
Anesthesia
Dissociative:
Opioids: Morphine, Fentanyl,
Ketamine is NMDA receptor
Sufentanil, Remifentanil
antagonist. Induces a
Opioids are frequently used
dissociated state. Dissociative
together with anesthetics due to
anesthesia provides sedation,
their analgesic property e.g.
amnesia, immobility.
Combination of morphine and
Lipophillic and cross BBB.
nitrous oxide provides good
Ketamine is employed mainly
anesthesia for cardiac surgery.
in children and young adults
Opioids are not good amnesics.
for short procedures.
A.E: Hypotension, respiratory
A.E: hypotension, Bradycardia,
depression, nausea, vomiting
Rashes, Resp. depress, GI dist.
Some risk renal
toxicity
Malignant
hyperthermia.
(Dantrolene should be
available for
emergency use when
needed)
A.E: diffusion hypoxia
Least hepatotoxicity.
Not depress
respiration.
Miscellaneous:
Propofol is an IV
sedative/hypnotic
onset is 30-40sec. 2-4
min half-life. used in
the induction or
maintenance of
anesthesia.
Supplementation with
narcotics for
analgesia is required.
It has replaced
thiopental as the first
choice for anesthesia
induction and
sedation, because
produces a euphoric
feeling in the patient.
A.E: Hypotension, ↓
in intracranial
pressure, Bradycardia.
 Local Anesthatics: Amides
Local anesthetics block nerve conduction of sensory impulses and in higher concentration motor impulses from periphery to the CNS. Delivery techniques include include
topical administration, infiltration, peripheral nerve block and neuraxial block. Chemically lipophilic group joined by amide or ester linkage to carbon chain.
Used as local anesthetic. A.E: Allergy , Urticaria
MOA: Block nerve conduction of Applied locally. Biotransformation In Severe hiccup hypotension,
Medium Acting sensory impulses from the periphery occurs primarily in liver and some In neuropathic pain bronchospasm,
Lidocaine to the CNS. Na+ ion channels are also in plasma ad kidney. Cause vasodilatation. coma, seizures ,
Long Acting blocked to prevent the transient Duration and onset of local By adding vasoconstrictor tissue necrosis,
Bupivacaine increase permeability. Stop sensation anesthetics influenced by several epinephrine the rate of local blurred vision
Rupivacaine in a limited area of the body. factors including tissue pH, nerve anesthetic absorption and tremors
In higher concentrations, stop motor morphology, concentration, pKa, diffusion decrease. C.I: In Bradycardia,
activity. and lipid solubility of drug. Some other therapeutic use heart block,
like Lidocaine , Antiarrhythmic Hypersensitivity, CHF.
Local Anesthetics: Esters
A.E: Allergy,
Urticaria, dizziness,
Short Acting tachycardia
Procaine Applied locally. ,angioedma, seizures,
MOA: Same as above.
Medium Acting Esters are Bio-transformed by Same as Above except anxiety, headache,
(All include a lipophilic group joined
Benzocaine Plasma cholinesterase (pseudo- antiarrhythmic Methemoglobinemia,
by an ester to a carbon chain)
Cocaine cholinesterase). Same as above. C.I: in bacterial
Tetracaine infection,
Ophthalmic
anesthesia

14
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)

Drug classification
googl
Inhibit the formation of dihydrofolic acid from PABA.
Drug compete with substrate for enzyme(folate synthetase)
• Natural penicillins:
Penicillin V, Penicillin G
• Semisynthetic:
Ampicillin , Amoxicillin
• Antistaphylococcal
penicillins:
Methicillin, Nafcillin,
Oxacillin
• Antipseudomonal penicillins:
Ticarcillin ,Piperacillin
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Chp-3 Chemotherapy
Antibacterials
Folate antagonists:
Sulphonamides
Mechanism of action pharmacokinetics Therapeutic use Adverse effects
Crystalluria
Hypersensitivity, rashes
Hematopoietic
Antimalarial disturbances
For toxoplasmosis Kernicterus
C.I: In newborns, infants
Nocardiosis
less than 2 months, in
Ophthalmic infection pregnant women
Topical infection, burn wound Resistance:
Well absorbed orally, I.V except In rheumatoid arthritis ↓ affinity for enzyme,
sulfasalazine.
efflux of drug bacteria,
Well distributed into the body also change the pathway for
in CSF, placenta,. folate synthesis
Metabolize in liver(acetylation)
Excreted in urine, and breast milk
Cell wall synthesis inhibitors:
penicillin (beta lactam )
Orally, I.V, I.M (combination is Hypersensitivity
Bactericidal Natural penicillins: Effect both
used) Diarrhea
Interfere with last step of bacterial but more for gram + & less
Ampicillin + salbactum, ticarcillin + Nephritis
cell wall synthesis(transpeptidation , gram – cocci ,bacilli,
clavulonic acid Neurotoxocity
crosslinking) so, osmotic lysis occurs, spirochete, choice for gas
Incompletely absorb after orally, (seizures)
inhibit penicillin binding proteins gangrene, syphilis.
effect intestinal flora, destroyed by Hematologic toxicities
which helps in synthesis cell wall and Antistaphylococcal penicillins:
stomach acid, should be given in (cytopenia)
maintenance of morphology, inhibit S. aureus
empty stomach, well distributed, Resistance:
transpeptidase, production of Antipseudomonal penicillins:
autolysins(degrade the old cell wall)
cross placenta, bones, CSF when
P. aeruginosa
Beta
inflamed, lactamase(hydrolyze
15
• Extendexd spectrum Nafcillin & oxacillin met. Bu liver, Extendexd spectrum the β-lactam ring)
penicillins: other Not metabolized, excreted in penicillins: more for gram- activity
Ampicillin , Amoxicillin urine by active tubular secretion, listeria monocytogenes ↓ permeability to the
probenecid inhibit their secretion drug
Altered PBPs
Cephalosporins: (β lactam)
• 1st generation: 1st generation:
Cefazolin, cefadroxil Skin & soft tissue infection Well tolerated but may
Orally and parenterally(mostly I.V, 2nd generation:
• 2nd generation: cause allergy, anaphylactic
Bactericidal I.M) Respiratory infections, sinusitis shock, skin rashes
Cefaclor, cefprozil, cefuroxime, cefoxitin
Bind to PBPs on bacterial cell Well distributed but first and 3rd generation: Resistance:
• 3rd generation:
membrane to inhibit bacterial cell second generation not penetrate Gram – infections, nephritis, Beta lactamase(hydrolyze
Cefixime, ceftriaxone,
wall synthesis by mechanism similar into CSF thyphoid, menengitis, nosocomial the β-lactam ring) activity
ceftibuten
to penicillins. Undergo hepatic metabolism infections but less common
• 4th generation: 4th generation: ↓ permeability to the
Less susceptible to β lactamase Renal excretion by active tubular
Cefepime Choice for nosocomial infections drug
mechanism
• 5th generation or advanced: 5th generation or advanced: Altered PBPs
Ceftaroline All
Carbapenems (synthetic β lactam)
Administered parenterally
Distributed to body tissues, Effective against gram+ ,gram- G.I distress, skin rashes,
Ertapenem , doripenem, Similar to penicillins Imipenem rapidly metabolized by renal
dehydropeptidase co-administered with
and anaerobes except at high doses CNS
imipenem, meropenem Less susceptible to β lactamase
cilastatin. ertapenem toxicity
Excreted in urine
Monobactam
I.V or I.M
Just against gram – Phlebitis, skin rashes,
Aztreonam Disrupt bacterial cell wall synthesis Metabolized by kidney
e.g P. aeruginosa abnormal liver function.
Excreted in urine
β lactamase inhibitors(miscellaneous)

They bind and inactivate the β-

Tazobactam, Sulbactam,
lactamases, themselves they have no
Clavulanic acid
significant ability against bacteria

16
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Protein synthesis inhibitors:
Aminoglycosides
Bacteriostatic or bactericidal
Diffuse through porin channel of organism cell, they bind
Effective against aerobic gram – bacilli, P. aeruginosa
to 30S ribosomal subunit, disturb its apparatus or lead to Polar ,not well
In tuberculosis, Tularaemia, Plague
misreading the genetic code absorbed orally,
must be
Adverse effects: ototoxicity, nephrotoxocity,
adminsitered neuromuscular paralysis, allergic reactions
Amikacin
Gentamicin parenterally,tissu
e conc. Is
Neomycin
subtherapeutic,
Streptomycin
penetrate in most
Tobramycin body fluids, cross
placenta, donot
cross
BBB.Excreted
unchanged in
urine

Bacteriostatic, Enter the organism by
passive diffusion, energy dependent
Doxycycline transport protein mechanism, bind
Minocycline reversibly 30S subunit, action
Tetracycline prevents binding of tRNA to the
mRNA-ribosome complex, inhibit
protein synthesis
Tetracyclines
Adequately absorbed after oral
ingestion, ↓ with dairy products
due to formation of chelates.well
distributed in liver kidney, bones
teeth skin, gingival fluid,in CSF,cross
placenta,
Not metabolized, some by liver,
excreted in urine .doxycline by
feces through bile
Chloramphenicol
Effective against gram+ ,gram-
bacteria, protozoa,spirochetes,
mycobacteria, chlamydia infection,
for acne
Resistance:↑ efflux of drug
,enzymatic inactivation, formation of
bacterial proteins that prevent the
binding to ribosome
G.I disturbance, effect
on calcified tissues,
hepatotoxicity,
phototoxicity, vestibular
dysfunction,
pseudotumor cerebri.
C.I: pregnancy, breast
feeding women, less
than 8 year children

Anemias, gray baby

Bind with 50S subunit of ribosomes,
inhibit protein synthesis at the
Chloramphenicol peptidyl transferase reaction, also
inhibit normal cell function like ATP
formation,
Against many type of
Given I.V, wideli distributed in body
organisms, chlamydia,
also in CSF, hepatic metabolism,
rickettsiae, spirochetes and
excreted in urine, also in milk
anaerobes
syndrome, liver enzyme
inhibitor
Resistance: :↑ efflux of drug
,enzymatic inactivation,
formation of bacterial
proteins that prevent the
binding to ribosome

17
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Macrolides or ketolides
G.I disturbances, cholestatic
Absorb orally, well distributed in Penicillin allergic jaundice, ototoxicity,
Azithromycin Bind irreversibly on 50S subunit, inhibit Resistance: :↓infflux of drug ,
body fluids, in prostate fluid in patients, H. influenza,
Clarithromycin translocation step of protein synthesis, :↑ efflux of drug ,enzymatic
macrophagse, except CSF, long half chlamydia, inactivation (methylase),
Erythromycin also interfere with other like
life, metabolized by liver,excereted H. pylori, S. pneumonia, prevent the binding to 50S
Telithromycin transpeptidation
in urine and feces mycobacterium ribosome, plasmid mediated
and estrases

Nucleic acid synthesis inhibitors

• 1st generation:
Nalidixic acid
• 2nd generation:
Norfloxacin, ofloxacin,
Ciprofloxacin
• 3rd generation:
Levofloxacin
• 4th generation:
Moxifloxacin
Quinolones(fluoroquinolones) man made antibiotics
Bactericidal, enter through porin channel,
Effective against gram-(E. Diarrhea, nausea,
Norfloxacin poor bsorb orally, short coli, P. aeruginosa, H. headache, dizziness,
show effect on DNA gyrase (topoisomerase-2
half life, ciprofloxacin 80% influenza,) tendon rupture,
in gram-) and topoisomerase-4 in gram +, by
gram + (streptococci) and arthropathy, glucose
inhibiting the topoisomerase-2 causes the bioavalibilty, Levofloxacin 100%
some mycobacteria dysregulation,
relaxation of supercoiling of DNA, ↑DNA bioavalibilty. Distribute well in body
for t.b, typhoid, cystic phototoxicity
strand breakage, inhibition of topoisomerase- fluids, high level in bone,urine, fibrosis, infectious Resistance:
4 impacts the chromosomal stabilization kidney, macrophages.excreted in diarrhoea, prostatitis, skin Altered target(mutation),
during cell division, thus interfere with the
urine except moxifloxacin by liver. infection, nosocomial ↓accumulation(alter porin
separation of newly synthesized DNA
infection,UTIs channel, ↑efflux pump)

Miscellaneous antibiotics
Potent inhibitors of bacterial
dihydrofolate reductase
Folic acid deficiency,
megaloblastic anemia,
Absorbed orally,concentratwe in leukopenia,
20-50 % more potent
Inhibitors of folate reduction prostate and vaginal fluid (due to granulocytopenia
than sulphonamides,
Pyrimethamine basic nature), little metabolized in Resistance:
used alone in UTIs, In gram – due to altered
Trimethoprim kidney, mostly excreted unchanged
prostatitis enzyme,
in urine
Trimethoprim ↓accumulation(alter porin
channel, ↑efflux pump)

Cotrimoxazole
(trimethoprim+ sulfamethoxazole)
Given orally, I.V, well distributed
Bactericidal cross BBB, some metabolized by
Block both enzymes. As above liver, excreted in urine in
metabolites and unchanged form
Antimycobacterial
Broad spectrum, effective in UTIs, respiratory tract
infections. Pneumonia, toxoplasmosis, salmonella
infections, skin and soft tissue infections
Adverse effects as above

18
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)

Prodrug activated by mycobacterial
catalase-peroxidase.
Inhibit mycolyic acid synthesis, disrupt
Isoniazid
cell wall
Target the enzyme acyl carrier protein
reductase & β-ketoacyl-ACP synthase
essential for mycolic acid synthesis.
First line drugs
Block RNA transcription by interacting
Rifamycins(rifam with β subunit of mycobacterial DNA
pin, rifabutin, dependent RNA polymerase
rifapentine Resistance:
Mutation in gene for above enzyme
Bacteriostatic ,mechanism is unclear but
Resistance occur Pyrazinamide
given in combination
if used single
drug so always
used in Bacteriostatic inhibit
combination arabinocyltransferase enzyme(involve in
formation of arabinogalactan, a
Ethambutol
component of mycobacterial cell wall
Resistance:
Mutation in gene for above enzyme
Well absorbed after orally,
distributed in all body fluid also in
CSF, met. By liver(acetylation)
In slow acetylators(3-4 hrs) in
fast(90 min). excreted in urine
Orally absob, distributed in all body
tissues fluids organsn also in
CSF(20%), met. By liver(undergo
enterohepatic circulation), excreted
through bile in feces, small %age in
urine
Orally absorb, well distributed also
in CSF, met. By liver ,ecxreted in
urine
Orally absorb, well distributed also
in CSF, met. By liver ,ecxreted in
met. And unchanged form in urine
Mycobacterium
tuberculosis & M.kansasii
Resistance: Hepatitis, peripheral
Mutation or deletion of neuropathy, CNS effects,
enzymes for drug hypersensitivity, rashes,
activation, mutation in fever
acyl carrier proteins,
overexpression of target
enzyme
For intracellular and Cyp450 enzyme inducer.
extracellular Hepatitis , nausea,
mycobacteria for M. vomiting, rashes, chronic
tuberculosis & liver disease, flu-like
M.kansasii, M. avium for symptoms fever, chill,
gram+ and – organisms myalgia, renal failure,
H.influenza, M.leprae shock
Liver toxicity, uric acid
Used in combination ,for retention, nongouty
short course treatment polyarthralgia, myalgia, G.I
irritation avoided in
of tuberculosis
pregnancy.
Optic neuritis, visual
Used in combination for acuity, red green color
treatment of tuberculosis blindness, retinal
damage, hyperuricemia

Aminiglycosides 1-Standad regimens

Fluoroquinolones 3-drugs isoniazid+rifampin+pyrazinamide for 2months than if HIV-ve patient
Macrolides 2 drugs isoniazid+rifampin for further 4 months
Second line
Amikacin 2- Alternative regimen
drugs
Ciprofloxacin isoniazid+rifampin for 9 months for fully susceptible person or isoniazid+ethambutol for 18 months(intermitent 4drugs)
capreomycin 3-if resistance occur
Aminosalicyclic isoniazid+ethambutol or streptomycin if resistance to isoniazid than
acid rifampin+ ethambutol or streptomycin for 6 months, multidrug resistance than 3 drugs for 18 months

19
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Urinary tract antiseptics
Given orally,distributed throughout For UTIs, during urinary
Methenamine decompose in acidic pH in G.I disturbance,
in body catheterization to reduce
urine thus produce formaldehyde, act albuminuria, hematuria
Methenamine Decomposes to foamaldehyde and bacteriuria, upper UTIs
locally and toxic for bacteria(given with rashes. C.I in renal
ammonium ions in bladder, liver Prevent infection in child
mandelic aci to make urine acidic) failure, no systemic
met. Ammonia to urea, bearing women and in
toxicity
Excreted in urine old age( E.coli)
G.I disturbance,
Against gram- (E.coli) neurologic problems,
Nitrofurantoin sensitive bacteria reduce
Given orally,distributed throughout gram+ cocci pulmonary fibrosis
Nitrofurantoin the drug into active metabolite that
in body, Excreted in urine (Staphylococcus C.I in renal failure and
damage bacterial DNA
saprophyticus) after 38 weeks or more
of pregnancy

Antifungal
Amphotericin B,
Drugs for systemic and Infusion related Fever,
Fingicidal and fungistatic Orally poor absorption, given I.V, Drug of choice in
subcutaneous mycosis chills, muscle spasms,
Bind with ergosterole in plasma well distributed in body fluids not in systemic mycosis(
• Alter the cell membrane shock like fall in blood
membrane, form channels, resulting in CSF,met in liver, excreted in bile candida, aspergillus,
permeability pressure, nephrotoxic,
leakage of electrolytes and small and urine blastomyces)
polyene neurotoxic
molecules which causes cell death.
Amphotericin B,
Azoles
fluconazole, ketoconazole,
Azoles Rarely used in systemic
voriconazole, itraconazole,
Inhibit the C-14 α-demethylase,thus mycosis due to toxicity,
posaconazole
inhibiting the demethylation of Posaconazole (candida,
• Block nucleic acid synthesis Rashes, vomiting
lanosterol to ergosterol(principal sterole Orally different bioavailibility, aspergillus, Rhizopus)
flucytosine diarrhea, hepatotoxicity,
of fungal cell membrane) distributed to most body fluid , not Itraconazole (choice in
• Cell wall liver CYP450 enzyme
in CSF except fluconazole, met. By blastomyces and
inhibitor(echinocandins) inhibitors
liver, ecxreted in urine except sporothrix and
Micafungin C.I in
ketoconazole(bile) chromoblastomycosis)
Anidulafungin pregnancy(teratogenic)
Fluconazole( choice in
caspofungin
oropharyngeal and
esophageal candidiasis)

20
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Flucytosine
Converted to 5-flurouracil and inhibit the thymidylate synthase, thus
inhibiting the DNA synthesis
Echinocandins
Fungicidal , inhibit the synthesis of
β(1-2)glycan, a critical component of
fungal cell wall
Drugs cutaneous mycosis
• Disrupt microtubule function:
Griseofulvin
• Alter cell membrane
Permeability:
Nystatin
Miconazole and other
topicalagents(clotrimazole,
butaconazole)
Squalene epoxidase inhibitor
Terbinafine
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Not effective orally, given as I.V,met by
liver, excreted in urine and feces
Griseofulvin
Nystatin
Same as amphotericin B
Miconazole and other topical agents act
like-wise azoles given above.
Terbinafine
21
Narrow spectrum use Bone marrow
with amphotericin B to depression,
produced synergistic thrombocytopenia,
effect neutropenia
Absorb orally, ↑with fatty food, In dermatophytic
Enzyme inducer,
distributed to stratum corneum, infection of skin and hair,
headache, mental
bind with keratin,met. In liver and ring worm(tinea corporis,
confusion, G.I irritation,
excreted in bile and urine tinae pedis, tinea barbae)
Not well absorb , used topicaly
Nausea, vomiting, bitter
only, not met. Excreted unchanged Use in candidiasis
taste
form in feces
Broad spectrum in topical
Act topically, not absorbe Dermatitis, edema
infections
Oral and topical preparations are
availible, first pass met. In Trichophyton rubrum,
Bioavailibility 40%, extensively T. mentagrophytes G.I disturbance, rash,
protein bound deposited in skin May be given in other headache
and fat tissues, met. By liver. topical infections
Excreted in urine

• Drugs for respiratory virus
infections:
Neuraminidase inhibitors
Oseltamivir, zanamir
Inhibitor of viral uncoating
Amantadine, rimantadine
Guanosine analog
Ribavirin
Drugs for treatment of hepatitis:
Interferon, Adefovir, lamivudine
Drugs for herpes & cytomegalo
virus infections
Cidifovir, ganciclovir, acyclovir,
fomivirsin
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Neuraminidase inhibitors
Neuraminidase is requir for virus life
cycle and for release of new virion( drug
inhibit the enzymes)
Inhibitor of viral uncoating
Interfere with viral M2 proteins, block
uncoating, prevent viral release from
infected cell
Guanosine analog
Drug firstly phosphorylated, and inhibit
GTP formation, prevent viral mRNA
capping and block the RNA dependent
RNA polymerase
Interferon
Not well known(but induce host enzyme
that inhibit RNA translation)
Adefovir
Nucleotide analog,phosphorylated by
cellular kinase and inserted intio viral
DNA, inhibit chain elongation and
replication
Lamivudine
Cytosine analog, phosphorylated, inhibit
the HBV, RNA dependent DNA
polymerase.
Acyclovir
22
Antiviral
Oseltamivir orally,prodrug
,converted to active form by liver,
zanamir by inhalation, both not
met. Excreted in urine Against influenza type A & G.I upset, CNS
Well absorb orally, distributed in B,Ribavirin broad spectrum effects(amantadine)
body tissues , cross BBB enter in (RNA & DNA viruses) Ribavirin(↑bilirubin)
CNS, not met. Excreted unchanged Resistance: Precautions
in urine Change M2 protein, Asthma,COPD,
mutation in gene for pregnancy, nursing
Given by inhalation & orally, enzyme(Neuraminidase) mother
distributed in body tissues ,not fully
met. By liver , excreted in urine
Not given orally, given parenterally,
little active in plasma,met by liver,
small excretion in urine
Against hepatitis A,B,C,D
and E (specially for
Well absorb orally, well distributed, Flu like symptoms(fever,
hepatitis B,C) chronic
drug is excreted in urine by kidney. chill, myalgia) G.I upset,
hepatitis, cirrhosis,
Headache, dizziness,
hepatocellular
carcinoma,
Well absorb orally, well
distributed,not met, excreted
unchanged in urine.
Well absorb orally, I.V, by topically,
well distributed, partially met. drug Prototype anti
Topically local irritation,
is excreted in urine by tubular herpetic(herpes simplex
headache, G.I upsey
secretion and by glumerular virus-1,2, varicella-zoster)
filtration.
 Ganciclovir orally, I.V, well distributed in CSF, met.by Carcinogenic
Against cytomegalo virus
Similar to acyclovir but at the end inhibit liver and in intestine, drug is excreted in ,embryotoxic and
urine by tubular secretion and by
infections(CMV)
DNA polymerase, results in chain teratogenic in exp.
termination glumerular filtration. animals

NRTIs
Analog of riboside, phosphorylated,
incorporated in DNA, block DNA chain
elongation, absorb orally, distributed in
body tissues, met in liver,excreted in urine NRTIs
Pancreatitis, lipoatrophy,
NNRTIs liver toxicity, acidosis,
• Drugs for HIV infections(AIDS) Non-competitive inhibitor of HIV-1 RT, hepatomegaly
Nucleotide or nucleoside reverse change the enzyme str. Hence Enzyme NNRTIs
inhibition, absorb orally, distributed in body
transcriptase inhibitors.(NRTIs) Hypersensitivity,
tissues also in CNS, extensively met by
Zidovudine, emtricitabine, tenofovir, liver,excreted in urine necrolysis,
lamivudine hepatotoxicity, insomnia,
Protease inhibitor headache, depressive
Reversible inhibitor of HIV aspartyl Treatment of HIV,
Non-nucleoside reverse disorder.
protease(used for plyprotein to essential ↓morbidity and
transcriptase inhibitors.(NNRTIs) Protease inhibitor
enzymes) so lead to non-infectious virion mortality in AIDS
Etravirine, nevirapine production, G.I upset, diabetes,
patients, restoration of
absorb orally↑with fatty food, bound to hypertriglyceridemia,
plasma proteins, distributed in body
CD4 cells, in
Protease inhibitor hypercholesterolemia,
tissues, extensively met by liver,excreted in immunocompetance of
Saquinavir, tipranavir, atazanavir breast enlargement,
urine host, always used in
headache, fatigue
combination to prevent
Fusion/entry inhibitors Fusion/entry inhibitors Fusion/entry inhibitors
resistance
Maraviroc(chemokine receptor Drug bind with transmembrane Pain, erythema,
CCR5 antagonist), enfuvirtide glycoproteins gp41, inhibit the bindind of induration, nodules at inj
viral cell with host cell, Maraviroc(orally),
site(enfuvirtide)
enfuvirtide(subcutaneous), met by
Integrase inhibitors(integrase CYP450,some time extrahepatic Integrase
strand transfer inhiobitors, INSTIs) hydrolysis,excreted in urine, inhibitors(INSTIs)
Raltegravir Muscle pain,
rhabdomyolysis,
depression, suicidal
Integrase inhibitors(INSTIs) ideation, nausea,
Inhibit the insertion of proviral DNA into
host cell by binding with the host cell DNA

23
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Antiprotozoal:
Anti-malarias
Pre-erythrocytic , exo- Nausea, vomiting ,
• Tissue schizonticide
epigastric distress,
Primaquine Primaquine Well absorb orally, wiedly erythrocytic,
haemolytic anemia in
• Blood schizonticides Mechanism not clear, said to act as distributed, met in liver, sloely gametocytic,
G6PD deficiency,
Chloroquine, Mefloquine, quinine, oxidant, which act as schizonticidal action release in urine Never used to treat and methaemoglobinemia
quinidine , artemisinine, pyrimethamine prevent malaria C.I in pregnancy, in children
Use to treat erythrocytic form of malaria
Chloroquine

Skin rashes, blurred

vision, G.I disturbances,
headache

Artemisinine

Use to treat erythrocytic

Oral, rectal,I.V, I.M prep. Are G.I disturbances, QT
form of malaria (againt
availible, well absob, met by prolongation,
quinine resistant strains
liver,excreted in bile neutropenia
of malaria)

Pyrimethamine

Absorb orally, bind to plasma

membrane, accumulate in liver, Both blood schizonticide Megaloblastic anemia,
lungs ,kidney.met by liver, excreted and sporonticide rashes, teratogenic effect
slowly in urine

Cinchonism(tinnitus,
Well absorb orally , well distributed
Quinine Use to treat erythrocytic vertigo, blurred vision)
in body, cross placenta,met by liver,
Similar to chloroquine form of malaria hypoglycemia,
excreted in urine
hypotension
24
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)

• Luminal amoebicides
Idoquinol, paromomycin
• Systemic amoebicidal
Dehydroemetine, emetine,
chloroquine
• Mixed amoebicides
Meteronidazole, tinidazole
Mixed amoebicides
Meteronidazole
• Drugs for the treatment of
Nematodes:
Mebendazole,thiabendazole
diethylcarbamazine,ivermectin,
pyrantel pamoate
• Drugs for the treatment of
cestodes
Niclosamide, Albendazole
• Drugs for the treatment of
Trematodes
Praziquantel
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Antiamebiasis
Effective against the luminal trophozoite and cyst forms
Luminal amoebicides Cryptosporidiosis, giardiasis Diarrhea, rashes,
Mechanism of Idoquinol is unknown
peripheral neuropathy,
Mechanism of paromkomycin is similar
optic neuritis,
to aminoglycoside
Systemic amoebicidal Used against amebiasis, Emesis, ECG changes,
Due to bitter taste of
Chloroquine given above Liver abscesses, eliminate tachycardia, itching,
Dehydroemetine given I.M,
Dehydroemetine inhibit protein synthesis trophozoite, malaria, not muscle weakning and
excreted in urine
by blocking the chain elongation for luminal trophozoite , stiffness
Choice for both intestinal and extraintestinal amebiasis, trichomonas vaginitis
G.I disturbances, metallic
taste, allergic reactions,
CNS effects, vertigo,
confusion , more effects
if used with alcohol
Antihelminthic
Effective against
G.I disturbances, nausea,
Mebendazole intestinal
Used orally, poorly absorbed, highly vomiting, diarrhea,
Inhibit the assenbly of microtubules in nematodes(round worm,
bound to plasma proteins, met. In rashes, drug fever,
parasite and block the glucose uptake, hook worm, pinworm,
liver, overdose excreted in urine abdominal pain
affected parasite is expelled in feces whipworm) and mixed
C.I in pregnancy
worm infestations
25
 Ivermectin
Choice for Dangerous mazzotti
Target glutamate-gated chloride channal
Well absorbe orally, distributed in onchocerciasis, (kills reaction(fever,
receptors, ↑ chloride influx, leading to
body tissues not cross BBB, met. By microfilariae not the headache, dizziness,
hyperpolarization, paralysis and death of
liver , excreted in urine adult worm) scabies, somnolence,
worm
pediculosis hypotension)
pyrantel pamoate

G.I disturbances, nausea,

Effective against intestinal nematodes(round worm, hook vomiting, diarrhea
worm, pinworm, whipworm) and mixed worm infestations

Albendazole G.I disturbances, nausea,

Similar to mebendazole vomiting, diarrhea, hair
Uses also similar(hydatid disease also) loss, hepatic dysfunction

Praziquantel Dizziness, malaise,

Well absorb orally, distributed in
↑ permeability to Ca+2, causes
body tissues , cross BBB, met. By
contaction of parasite and death
liver , excreted in urine
Choice for
headache, G.I upset, C.I
schistosomiasis,
for ocular cycticercosis
taeniasis, cysticercosis
(damage eye)

Anti-leishmanials

pancreatitis, ↑ liver
Sodium stibogluconate poorly absorb orally,I.V, distributed
Sodium stibogluconate Leishmania(due to enzymes, arthralgia,
Kill parasite by inhibiting glycolysis oe in extravascular tissue, met. Is
Miltefosin sandfly) myalgia, G.I upset, pain
effect the DNA metabolism minimal , excreted in urine
at inj.

26
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Anti-Neoplastic drugs(anticancer)

Nausea, Vomiting,
Capicitabine
Orally well absorbed Diarrhea, renal
It Converted into 5-florouracil and inhibit In breast cancer,
Metabolize in liver impairment ,
the thymidylate synthase enzyme and in Colorectal cancer,
Excreted in Urine and also exhaled hepatotoxicity
result cell death occur. Against some tumors
with CO2 C.I: Pregnany, Lactating
mothers

Used in combination
Administered by Oral, IM, IV and
against
Intrathecal route.
Acute lymphocytic Nausea, Vomiting,
Methotrexate Variably absorbed at low doses
anemia, Diarrhea, Urticaria,
It inhibits the DHFR and THFR enzyme from the GI tract,
choriocarcinoma, breast Alopecia, Renal Damage,
Anti-Metabolites (All are cell cycle and depressed the synthesis of RNA, DNA Distributed to intestinal epithelium,
cancer, head and neck Hepatic Toxicity,
specific, S-Phase) and proteins, ultimately cell death liver, skin.
carcinoma. Pulmonary toxicity,
Capicitabine occurs. Cannot cross BBB.
As single dose against Neurological toxicity,
Methotrexate Metabolize in liver, excreted in
sever psoriasis, C.I= in pregnancy
(Folate antagonist) urine.
rheumatoid arthritis,
6-Mercaptopurine,
Crohn’s disease.
6-Thio-guanine (Purine Analog)
6-Mercaptopurine Incomplete absorbed after oral Majorly in acute Major is bone marrow
5-Fluorouracil (5-FU)
Formation of nucleotide analog, administration, widely distributed lymphoblastic anemia, depression, Nausea,
(Pyrimidine analog)
Inhibition of Purine synthesis, in body except CSF, metabolize in neoplastic disease Vomiting, Diarrhea,
Cytarabine
Incorporation in nucleic acid. liver converted into 6- Also have Anorexia, Hepatotoxicity
Gemcitabine
This result in synthesis of non-functional mathylercaptopurine (Inactive) in immunosuppressant in the form of jaundice.
RNA and DNA. liver and excreted by kidney. action C.I= in pregnancy
5-Fluorouracil (5-FU)
Enter the cell through a carrier mediated
transport system , converted into the Hand-foot syndrome.
deoxynucleotide (5-floro deoxyuridine Given IV and topically, Penetrate In Treating solid tumor, (Same as above)
monophospate. 5-fdUMP acts as a well into all body tissue including Colorectal cancer, Resistance: is
pseudo substrate and is trapped with the CNS, Metabolize in liver, kidney, Breast Cancer, encountered when the
enzyme and its coenzyme in complex lungs, Gastric carcinoma, cell have lost their ability
that cannot proceed to release product. Can cross BBB Ovary Cancer, to convert 5-FU into its
As a result DNA synthesis decreases due Excreted in urine Skin cancer. active form.
to lack of thymidine leads to cell death. C.I= in pregnancy
It also incorporates into RNA.

27
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)

Anti-Biotic
(All are cell cycle non-specific)
Doxorubicin, Daunorubcin,
Idarubicin, Epirubicin,
Dactinomycin
Bleomycin (In G2 phase)
Alkylating agent
(All are cell cycle non-specific)
Cyclophosphamide & Iphosphamide
Nitrosourease
(Carmustine & Lomustine)
Dacarbazine
Temozolamide
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
Majorly in acute non- Sever Meylosuppression,
Cytarabine Not effected orally,Given IV,
lymphocytic leukemia in Paralysis,
It effectively Inhibit the DNA polymerase intrathecally.Distribute throughout
combination with Liver dysfunction,
enzyme and also incorporated into the body but not enter into CNS. duanarubicin, nausea, vomiting.
nuclear DNA and retard DNA elongation. Excreted in urine. In meningeal leukimia
Meylosuppression,
Gemcitabine In metastatic
Infused IV. rashes, proteinuria,
Inhibit DNA synthesis by incorporating adenocarcinoma of
Metabolize in liver hematuria, Nausea ,
into growing strand that ordinary would pancreas,lung cancer,
Excreted in urine Vomiting, Diarrhea,
contain cytosine. Some tumors
alopecia
Doxorubicin, Daunorubcin, Idarubicin,
In Sarcomas, carcinomas, Cardio toxicity,
Intercalation in the DNA , Administered by IV inactive in GI
Breast cancer Bone marrow suppression
Binding to cell membrane and alter the tract, bind to plasma proteins and
Lungs cancer Stomatitis,
function of transport process. distributed well in body and cannot
Lymphomas Skin pigmentation
Generate O2 free radicals which reduce cross BBB or testes. Metabolize in GI disturbance
Acute Lymphocytic
the molecular O2 of cell. liver and majorly excreted in bile. C.I: Heart patient
leukimia
& inhibit topoisomerase 1 & 2.
In Wilm’s tumors, Bone marrow
Dactinomycin
Administered IV, distribute too Sarcoma, Carcinoma suppression
The drug intercalates into the minor
many tissues but not in CSF. Mainly Breast cancer Immnosupression,
groove of the double helix between
metabolize in liver. Excreted in bile Resistance: due to Stomatitis,
guanine-cytosine bases pair of DNA, and
and some in urine. increase efflux of Alopecia, GI disturbance,
it also hinders DNA synthesis and also
antibiotic from the cell Inflammation.
inhibit topoisomerase 2.
via p-Glycoprotein.
Administered by number of routes,
Pulmonary toxicity,
Bleomycin IM, IV, subcutaneously, In testicular cancer,
Cough , fatal fibrosis,
Intercalation & scission of DNA, resulting intracavitary. Squamous cell
Alopecia,
in stand breakage and chromosomal Hydrolyse highly in liver and spleen carcinoma,
Hyper pigmentation,
aberrations. and most of parent drug excreted Lymphomas
Risk of fever and chills.
unchanged in urine.
Cyclophosphamide & Iphosphamide Leukocytosis, amenorrhea,
First biotransformed into hydroxylated Administered IV and orally, oral In neoplastic disease, Aspermia, neurotoxicity,
intermdeidate primerly in liver by CYP450 route is preferred. Burkitt Lymphoma, alopecia, bone marrow
then undergo breakdown to form active Can cross BBB. Breast cancer depression, GI disturbance.
compound phosphoramide musterd ans Excreted into feces or urine by Nyphrotic syndrome Resistance: Due increase
acrolin which react with DNA and cause glomerular filtration. Rheumatoid arthritis DNA repair, decrease drug
cytotoxicity. permeability.
28
Other Alkylating agent(Melphalan, Carmustine & Lomustine
Clorambucil, Busulfan) Carmustine IV In treatment of brain
Exert cytotoxic effects by alkylation that Delayed hemapoietic
Lomustine Orally tumors and limited use.
inhibits the replication, RNA and protein depression, aplastic
Distribute widely in the body, Resistance: Due to DNA
synthesis. marrow, renal toxicity,
Can cross BBB. Metabolize in liver repair,
Also inhibit some key enzymatic process pulmonary fibrosis
excreted through kidney and in Reaction of drug with
by carbamoylation of amino acids in
urine. thiols.
proteins.
Dacarbazine
Undergo biotrnasforamtion to form
Nausea, Vomiting
active metabolite, Administered IV,
In treatment of Meylosuppression
MethyTriazenoImidazole Carboxamide Metabolize in liver
melanoma Hepatotoxicity,
(MTIC) which is responsible for Excreted in urine
neutropenia
methylation of DNA on 6 position of
guanine

Temozolamide
Taken orally, Can cross BBB
Same as Dacarbazine In treatment of gliomas,
Metabolize in liver Same as Dacarbazine.
Also inhibit the repair enzyme , Anaplastic astrocytomas
Excreted in urine
O6- guanine DNA-alkyltranferase

Melphalan, Clorambucil, Busulfan These In multiple myeloma, hematologic toxicity,

Given Orally, Metabolize in liver
are bifunctional Alkylating agent and Chronic lymphocytic & Pulmonary fibrosis,
Excreted in urine
cause alkylation and cytotoxicity. granulocytic leukemia And Same as Above

Phlebitis or cellulitis,
Vinblastine(VBL),Vincristine(VX), Administered by IV, In acute lymphoblastic alopecia, Nausea,
Vinorelbine(VRN) Metabolize in liver leukemia in children, Vomiting, Diarrhea,
(Specific for M-phase)Block mitosis in M- Excreted in bile and feces. Wilm’s tumor, sarcoma, Bone marrow
phase and block the ability of tubilin to Resistance: Due to enhanced efflux Hodgkin’s and Non- suppression,
Microtubule Inhibitors
polymerize form microtubules, results in of VBL, VX, VRN and alteration in Hodgkin’s lymphomas, Myelosuppressent,
(All are cell cycle specific)
dysfunctional spindle apparatus. tubilin structure. lungs cancer. ataxia
Vinblastine(VBL),
Vincristine(VX), Vinorelbine(VRN)
Paclitaxil & Docetaxil(Specific in G2/M
Paclitaxil, Docetaxil
phase)Bind reversible with β-tubilin Given IV, well distributed, Neutropenia,
subunit and promote polymerization and Cannot cross BBB, bradycardia, alopecia,
Same as Above
stabilization of polymer rather than Metabolize in liver Urticaria, dyspnea,
disassembly due to which stable non- Excreted in bile and eliminated in hypotension.
functional microtubules are formed and stool. C.I: Heart Patients.
results in cell death

29
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Trastuzumab
Administered IV
Exact mechanism unknown but may be
Used in combination with other Heart failure, abdominal
down regulation of HER-2 (Human In metastatic breast
drugs pain,
epidermal growth factor receptor protein cancer,
Cannot cross BBB. Back pain, headache,
2) expression, Gastric cancer,
Monoclonal Antibodies Metabolize nonspecifically into chills , dizziness, GI
Induction of antibody de pendent adenocarcinoma
Trastuzumab, smaller peptides and amino acids disturbance
cytotoxicity or decrease in angiogenesis
Rituximab, Very low renal excretion
Cetuxizumab,
Post transplant Hypotension,
Bevacizumad Administered IV
Rituximab lymphoma bronchospasm,
Used in combination with other
Binds to the CD20 antigen on the B- Chronic lymphocytic Angioedema, chills,
drugs.
lymphocyte which induces the cell leukimia fever,
Eliminated through
mediated cytotoxicity of B cells. Non-Hodgkin’s Tumor lysis syndrome,
reticuloendothelial system
Lymphoma leucopenia, neutropenia
GI disturbance,
Administered IV Ovarian cancer,
Nephrotoxicity,
Highly plasma protein binding, Testicular cancer,
Platinum Containing Compounds Ototoxicity,
Form highly reactive platinum complex Poorly penetrate BBB, accumulated Endometrial cancer,
(All are cell cycle non-specific) hypocalemia,
which reacts DNA and damaged the DNA. in kidney, intestine, testes Bladder cancer,
(Cisplatin, Carboplatin, Oxaliplatin) Hypocalicemia,
Metabolize in liver Colorectal cancer,
Neuropathy.
Excreted in Urine Gastric cancer

Tyrosine kinase inhibitors

Imatinib, dasatinib, nilotinib

Topoisomerase inhibitors
etoposidse

Steroids
Tamoxifen,
Aromatase inhibitors
Anastrazole, letrazole

Hydroxyurea CML (Chronic Myeloid

Miscellaneous Agents Interfere with conversion of Administered Orally Leukemia) Bone marrow
(All are cell cycle specific and acts in ribonucleotide to deoxyribonucleotide by Metabolize in liver Polycythemia suppression,
S-phase) inhibiting Well absorbed from G.I.T Psoriasis, Leukemia,
Ribonucleotide diphosphate reductase. Renal excretion is pathway of Ovarian cancer, Anemia,
This results in inhibition of DNA excretion. Melanoma Thrombocytopenia
synthesis.

30
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Immunosuppressants and immunostimulants

31
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 32
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 33
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 34
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 35
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 Non-steroidal anti-inflammatory Drugs(NSAIDS)

36
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 37
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)
 38
Best PDF Encryption Reviews
By Hafiz Muhammad Attaullah & Aqib Razzaq (session 2016-21)