Pharmacology
Lecture 3 (Metabolism)
Drug
Function
Allopurinol
Levodopa
Lindocaine
1. Phenytoin
2. Oral contraceptive
Rifampicin
1. Erythromycin
2. Warfarin
Ketoconazole
Chloramphenicol
Inhibitor of xanthineoxidase and used to treat gout.
Dopamine precursor (it get converted to dopamine).
Hydrolyzed by amidase and it’s used as local anesthetic.
It’s an enzyme inducer and it’s used as antiepileptic.
It’s an enzyme inducer and it’s used as anti TB.
It’s an enzyme inhibitor and it’s used as antibiotic.
It’s an enzyme inhibitor and it’s used as antifungal.
Causes Gray baby syndrome when there’s deficiency of Glucouronyl transferase.
Lecture 4 (Execration)
Drug
Function
Amphetamine
Aspirin
Aminoglycosidic
antibiotics
(gentamycin),
Penicillin, Lithium
Penicillin,
Tubocurarine
Digoxin, Thyroxin
Penicillin
Salicylates,
Sulphoamides,
Penicillin
Morphine, Atropine,
Quinine, Neostigmine
Morphine
Digoxin, Morphine,
Thyroxin.
Amoxycillin
Basic drug. We use acidification of urine by NH4Cl to increase execration of it.
Acidic drug. We use Alkalization of urine by NaHCO3 to increase its execration.
Drug
Vincristine
Colchicine
Neostigmine
Organophosphates
Local Anesthetics
Drugs execrated mainly by kidney.
Drugs of short plasma half-life.
Drugs of long plasma half-life.
Activly excecreted drug.
Acidic drugs.
Basic drugs (-ine).
Reachs steady state concentration after 3-5 half-lives.
Goes through Enterohepatic Circulation.
Patient needs to take (500mg) / 8 hours to maintain therapeutic level.
-Lecture 5Function
Target Tubulin and it’s an anti cancer drug.
Target Tubulin and used to treat gout.
The drug competes reversibly with the natural substrate (ACH) for the enzyme
(cholinesterase at MEP).
The drug competes irreversibly with the natural substrate (ACH) for the enzyme
(cholinesterase).
Block Na influx through Na channel in nerve fibers.
Sulfonylurea drugs
Block K+ out-flux via the K channels in pancreatic cells (K Channel Modulator).
Pindolol:
Propranolol*
Tubocurarine
Digitalis
Cocaine
Partial Agonist, produces less decrease in heart rate than pure antagonists
Antagonist
Blocks efflux of Na by Na pump
Blocks transport of catecholamines at synaptic cleft in CNS..
Lecture -6Drug
Function
Dimercaprol
Omeprozole & Hestamine
Phenobarbitone & Warfarin.
Chemical antagonism (reduce heavy metal toxicity).
Physiological antagonism.
Pharmacokinatic antagonism (Phenobarbitone accelerates hepatic
metabolism of warfarin).
Reversible competitive antagonism.
Irreversible competitive antagonism.
Atropine Vs. ACH
Phenoxybenzamine Vs.
Noradrenalin
Verapamil Vs.
Noradrenaline
-Lecture 8Function
Drug
Statins
Estrogen
Nitrates
Na Nitroprusside
Sildenafil –ViagraPropranolol*
Aliskiren
lisinopril
omapatrilate
candisartan
spirinolactone
Eplerenone
Anthypertensive drugs
NSAIDS **
Drug
Morphine
Diphenhydramine
Loratadine
Cimetidine
Non-competitive antagonism.
Express eNOS , CVS Cytoprotection. (it increases the enzymes that
synthesis NO).
Express eNOS , CVS Cytoprotection. (it increases the enzymes that
synthesis NO).
Act as NO donners, Venulodilators in angina.
Act as NO donners, Arteriolar dilator in hypertension.
Inhibit Selective PDE5 , Erectile dysfunction.
Inhibit activation of renin
Inhibit renin directly
ACE inhibitor
Vasopeptidase
ARBs
ADOSTERONE Antagonists
ADOSTERONE Antagonists
ACE Inhibitors ,VASOPEPTIDASE
 bradykinin mediated pain
-Lecture 9Function
Release histamine
Has sedating effect, used in Allergic conditions, Insomnia and Motion
sickness.
Used in Allergic conditions.
Treatment for peptic ulcers because it is an Inhibitor of gastric acid (HCl)
Betahistine
Corticosteroids
NSAIDs **
ex. Aspirin
Zafirlukast/zileuton
Carboprost
Latanoprost
Misoprostol
Drug
Barbiturates &
Contraceptive pills
NSAIDs
Isoprenaline
BetaAdrenoceptors
Amphetamine
Warfarin
Quinidine
Corticosteroids
Retinoid
Morphine
Penicillin
Sulphonamides
Local anesthetics
creams
secretion.
Treatment for vertigo in middle ear.
to inhibit the release of phospholipase A2
inhibit the release of Cyclooxygenase
inhibit the release of Lipoxygenase
Induce abortion in first trimester (first 3 months) and Treatment of
postpartum hemorrhages.
Eye drops in treatment of open angel glaucoma
Treatment of peptic ulcer.
Lecture -10Function
Pre-Receptor Events (Drug-Drug interaction) – (Barbiturates increase
metabolism of contraceptive pills)
Post-Receptor Events (Drug-Body interaction) - Activation of renin angiotensin
system to nullify antihepersensitive effects by ACH inhibitors.
Down regulation (decrease number of receptors) by activation of beta-receptors
to increase receptors recycling by endocytosis.
Binding Alteration (phosphorylation of receptors leads to decrease of activation
of AC to related ionic channel).
Exhaustion of mediators (depletion of mediator stores).
Leads to hemorrhage – Augmented (Type A)
1. Bizarre (Type B) type II hypersensitivity (Cytotoxic) – Hemolytic anemia
thrombocytopenia.
Chronic intake leads to osteoporosis – Continuous (Type C)
Produce side effect after long period of time – Delayed (Type D)
Withdrawal syndrome – End-of-Use (Type E)
Type I hypersensitivity (Anaphylaxis) – Urticarial, rhinitis, bronchial asthma.
Type III hypersensitivity (Immune complex) – Urticarial, fever, arthritis, and
enlarged lymph nodes.
Type IV hypersensitivity (Cell Mediated) – Contact dermatitis.