Pharmacology Flashcards
Define pharmacokinetics
Study of drug movement in the body/ effect of body on the drug
Define side effects
Unwanted effects of the therapeutic doses
Define agonist vs antagonist
Agonist: have affinity and maximal efficacy
Antagonist: have affinity and no maximal efficacy
Define clearance
Measure of the body’s ability to excrete the drug
Optimal effect exerted over narrow range of plasma drug concentration is …..
Therapeutic window phenomenon
Define drug efficacy vs drug potency
Drug efficacy: maximal effect that a drug may elicit
Drug potency : amount of drug required to produce a certain response
Define bioavailability
Fraction of the drug that reaches the blood.
Microsomal enzyme inducers (3)
Phenytoin
Phenobarbitone
Rifampicin
Drugs showing high first pass metabolism are (3)
Lignocaine
Propranolol
Salbutamol
Define first pass elimination
Metabolism of drug in liver,intestine/portal blood. + Excretion of drug into bile
T1/2 can determine (4)
Elimination time
Steady state plasma conc
Dosing rate
Maintainance dose
Egs of prodrugs (4)
Enalapril
Sulindac
Ticlopidine
Clopidogrel
Difference between zero order and first order kinetics
Zero order First order
1. Constant amount Constant fraction
2. t1/2 variable t1/2 constant
3. Rate of elimination Rate of elimination
independent dependent
Phases of clinical trials and it’s determination
Phase 1: Human pharmacology & safety
Phase 2: Efficacy, dose ranging.
Phase 3: therapeutic confirming
Phase 4: post marketing surveillance
Drugs causing osteoporosis (2)
- Steroid
- Heparin
Drugs with low safety margin (3)
Lithium
Aminoglycosides
Digoxin
Drugs causing hirsuitism (2)
Minoxidil
Phenytoin
Drugs causing extra pyramidal side effects (2)
Haloperidol
Levodopa
Hemolysis in G6PD deficiency caused by …(4)
Dapsone
Primaquine
Sulfonamides
Nitrofurantoin
Drug deposited in retina
Drug deposited in muscle
Chloroquine
Digoxin
Drugs causing hepatitis (4)
Halothane
Rifampin
INH
Pyrazinamide
Drugs causing intrahepatic cholestasis (2)
Phenothiazines
TCA
Egs of hepatotoxins (2)
CCL4
Paracetamol
Drug metabolised in liver (4)
Phenytoin
Erythromycin
Cimetidine
Diazepam
Drug metabolised in kidney
Penicillin G
Duration of action of a drug administered iv depends upon (5)
- Protein binding
- Clearance
- Distribution volume
- Lipid solubility
- Drug concentration
Effect of displacement of protein bound drug
Raises plasma level of that drug
Drug binding sites on protein are :
Non-specific- one drug can displace the other
Drugs bound to albumin (2)
Phenytoin
Warfarin
Phase 2 of drug metabolism involves (3)
Conjugation with glucoronide, sulfate, glutathione
Ach as a molecule can’t be used because
Uses of neostigmine/pyridostigmine (3)
It is rapidly degraded
Urinary retention
Ileus
Reversal of Nm blockade
Pupil in organophosphate poisoning
Rx for organophosphate poisoning
Pin point
Atropine + pralidoxime
Use of atropine (3)
- Rx of bradyarrhythmias
- Early mushroom poisoning
- Organophosphate poisoning
Alpha 1 agonist egs (2)
Phenylephrine
Methoxamine
Alpha 2 blockers
Yohimbine
Mirtazapine
Egs of beta agonists
Isoproteronol ( beta 1= beta 2)
Dobutamine (beta 1> beta 2)
Egs of beta 2 agonist (3)
- Salmeterol
- Terbutaline
- Ritodrine
Timolol is c/i for …..(2)
Heart block
Asthma
Shortest acting beta blocker
Esmolol
Egs of 5HT 1 A and 5HT 1 B agonist
5HT 1A agonist : Buspirone
5HT 1B agonist : sumatriptan
Eg of 5HT 4 agonist.
Egs of 5 HT 2A antagonist (2)
Cisapride
Cyproheptadine
Ketanserin
Egs of 5HT 2A/2C antagonist
Egs of 5HT 3 antagonist
Clozapine
Ondansetron
2 roles of PG
Cytoprotective for stomach
Contract uterus
Rx for NSAID induced ulcer
Thromboxane is a …….
Misoprostol
Platelet aggregator
Uses of alprostadil (2)
PGE1
Causes vasodilation
Useful in erectile dysfunction
Uses of dinoprostone (3)
PGE 2
Contraction of uterus
Abortificant
Cervical ripening
Eg of irreversible COX inhibitor
Egs of selective COX 2 inhibitor
They lack ……
Aspirin
Lumiracoxib
Valdecoxib
They lack anti platelet action
Nimesulide and diclofenac are …..COX inhibitors
Preferential COX 2 inhibitor
NSAID with good tissue perfusion
NSAID with good conc in synovial fluid
Ketorolac
Diclofenac
Non narcotic non steroidal drug is ….
Acts on ….
Ketorolac
Opioid receptors
Indapamide is a …….drug
Side effects of the above . (2)
Thiazide diuretic drug
Hyperglycaemia
Hypercalcemia
Important feature of thiazides
Used in rx of hypercalciuria, but they themselves cause hypercalcemia and renal calculi
Furosemide is a …….derivative
Side effects of furosemide (3)
Sulfamoyl derivative
- Hyperuricemia
- Hypocalcemia
- Hyperlipidemia
Spironolactone antagonises ……
Sodium retaining effect of aldosterone
Active metabolite of spironolactone is …..
Caneronone
MOA of mannitol
Increases ECF and renal blood flow especially to medulla
C/I of mannitol (3)
- Acute tubular necrosis
- Anuria
- Pulmonary Edema
Effect of metformin on glucose metabolism (2)
- Increased glycolysis
- Decrease gluconeogenesis
Special feature of metformin (2)
Does not cause weight gain, hence used in obesity
Obesity is not a c/I
Egs of alpha glucosidase inhibitor (2)
Acarbose
Miglitol
MOA of Acarbose , miglitol (2)
- Reduces fibrinogen level
- Decrease progression of impaired glucose tolerance to overt disease
Special feature of Acarbose,miglitol
Do not cause hypoglycemia
Features of tolbutamide (3)
It’s a sulfonylureas
Causes hypoglycemia that is
Severe
Prolonged for days
Fatal - elderly and heart failure
Effect of pioglitazone (2)
Acts by binding to PPARS
Increases insulin sensitivity
t1/2 of insulin
Difference of human and pork insulin
5 minutes
Differs by 1 amino acid
Humulin is ……
Human insulin
Max mineralocorticoid activity shown by ….
Max glucocorticoid activity shown by ….
- Aldosterone
- Dexamethasone
Androgen receptor blocker:
Anti-estrogen drug
Cyproterone
Clomiphene
Tamoxifen decreases……
Agents used for ca breast (3)
FSH
- Tamoxifen
- Exemastine
- Letrozole
S/E of danazol (3)
- Acne
- Weight gain
- Occasionally hot flashes
Flutamide and nilutamide are …..
Use of flutamide
Antiandrogens
Metastatic prostate cancer along with GNRH analogues
MOA of theophylline and doxofylline (5)
- Inhibit PDE4
- Increase CAMP conc
- Blocks adenosine receptors
- Beta 2 agonist
- Stimulator of mucociliary movement
Factors decreasing theophylline levels (2)
- Smoking
- Enzyme inducers
Factors increasing plasma levels of theophylline (3)
- Erythromycin
- Ciprofloxacin
- Cimetidine
MOA of monteleukast (2)
- CysLT1 receptor antagonist
- Blocks action of leukotriene D4 on cysLT1 receptor in lungs
Uses of monteleukast (3)
- Used in maintenance therapy of asthma
- Relief of seasonal allergies
- Not used in acute attacks
Steroid in asthma
Act by ….(3)
No role in acute attacks/ status asthmaticus
1. Anti I.F / reduce airway I.F
2. Increase lipocortin levels
3. Blocks phospholipid breakdown
Commonly used steroids in asthma (3)
- Budesonide
- Triamcinolone
- Fluticasone
S/E of parenteral steroid
Zafirlukast is taken …..
Posterior subcapsular cataract
Once daily
Egs of anticholinergic bronchodilators (2)
Ipratropium
Tiotropium
Drugs which inhibit cross linking (transpeptidases) and impair cell wall synthesis (5)
- Penicillin
- Cephalosporins
- Vancomycin
- Imipenem
- Aztreonam
Drugs binding to 30S ribosomal units and inhibiting protein synthesis (2)
- Streptomycin
- Tetracycline
MOA of trimethoprim
Inhibit nucleotide synthesis of tetrahydrofolate
Penicillinase resistant drug is ….(2)
Methicillin (acid labile )
Cloxacillin
Quinupristin/dalfopristin are ……
(Bactericidal/bacteriostatic)
Used in …..
Bacteriostatic
Vancomycin resistant enterococcus fecalis
Imipenem is inhibited by ……
Dihydropeptidase
Special feature of aztreonam
Can be safely given to patients allergic to penicillin and related group of drugs - coz they lack cross reactivity
Egs of glycopeptide antibiotics (2)
Vancomycin
Teicoplanin
S/E of vancomycin
DOC for MRSA infection
Red man syndrome
Metronidazole 1st
Vancomycin 2nd
Drug used to rx pseudomembranous colitis
Cefoperazone has ……activity
Vancomycin
Antipseudomonal activity
Azithromycin is effective against (4)
- Chlamydia
- Mycoplasma
- Ureaplasma
- Legionella
Macrolides cause GIT distress why?
Drug used for penicillin allergies
Coz they stimulate motilin receptors
Erythromycin
Complications arising from outdated tetracycline
S/E of doxycycline
Fanconi’s syndrome
Photodermatitis
Tetracycline causing hyperpigmentation
Minocycline
S/E of tetracycline (3)
- Teratogenic
- Superinfection
- Tooth discoloration
MOA of chloramphenicol
MOA of clindamycin
Bind to 50S subunit
Block elongation of peptide chain
Bind to 50S subunit and inhibit protein synthesis
MOA of aminoglycosides (3)
- Inhibit translation
- Bactericidal
- Distribution only extracellular
Streptomycin is used in …..
S/E of aminoglycosides
Plague/tularemia
- Teratogenic
- Ototoxic
- Vestibulotoxic
- Nephrotoxic
- Causes Nm blockage- should not be used for rx of myasthenia gravis