PHARMACOLOGY Flashcards
Basic Drug better absorbed from
Small Intestine
Acidic Drug better absorbed from
Stomach
Eg Aspirin
Aspirin poisoning
forced alkalisation by Sodium bicarbonate or Acetazolamide
Morphine poisoning
Forced acidification by Ascorbic acid or Ammonium chloride
Antidote IV NALOXONE (DOC) and oral NALTREXONE
Henderson Hesselbach Equation
pka=ph + log ionised A/unionised A
p-gp inhibitors
Verapamil
Amiodarone
Cyclosporine
Itraconazole
Nifedipine
Erythromycin
Quinidine
p-gp inducers
Rifampicin
St. John’s wort
phenytoin
Carbemazepine
Bioequivalent
Same drug, same dose, same conte with <20% difference in BA
No role for hemodialysis
Amphetamine
Verapamil
Opioids
Imipramine (TCA)
Digoxin
Diazepam-Strong plasma binding protein
AVOID DIALYSIS AVOID-Large Vd drugs
Vd
Vd=Total dose / plasma concentration
Loading dose
Loading Dose= Vd x Target plasma concentration
Half life
0.693 X Vd / CL
Clearance
Rate of Elimination / plasma Concentration
maintenence dose
Maintanence dose = CL X target plasma concentration
Acidic Drugs bind to
Albumin
Acidic Drugs bind to
Albumin
Acidic Drugs bind to
Albumin
Basic drug bind to
Alpha 1 acid glycoprotein
Salicylate displace
TOLBUTAMIDE
WARFARIN
Aspirin displace
Thyroid hormone
Aspirin displace
Thyroid hormone
Sulphonamide displace
Bilirubin so Kernicterus in newborns.
Blood brain barrier absent in
pituitary
Pineal
CTZ
Median Eminence
Blood brain barrier absent in
pituitary
Pineal
CTZ
Median Eminence
Drugs that do not cross BBB
Streptomycin-cross placenta
Neostigmine
Glycopyrrolate- anticholinergic
Dopamine
Ultrashort acting barbiturate in Induction of GA
Thiopentone Sodium
Ultrashort acting barbiturate in Induction of GA
Thiopentone Sodium
Ultrashort acting barbiturate in Induction of GA
Thiopentone Sodium
Active metabolite of Diazepam
Oxazepam
Active metabolite of Spironolactone
Canrenone
Primidone active metabolite
Phenobarbitone
Primidone active metabolite
Phenobarbitone
Phenecitin active Metabolite
Paracetamol
Phenecitin active Metabolite
Paracetamol
Inactive drugs
Levodopa-Dopamine
Minoxidil - Minoxidil sulphate
Enalapril- Enalaprilat
Dipivefrine-Epinephrine
Methyl DOPA-Methyl Norepinephrine
Inactive drugs
Levodopa-Dopamine
Minoxidil - Minoxidil sulphate
Enalapril- Enalaprilat
Dipivefrine-Epinephrine
Methyl DOPA-Methyl Norepinephrine
ALE I which are not prodrugs
Captopril & Lisinopril
most common phase I reaction
Oxidation
Most common phase II Reaction
Glucoronidation
Most common phase II Reaction
Glucoronidation
PCM intermediate
NAPQI-highly hepatotoxic
PCM intermediate
NAPQI-highly hepatotoxic
microsomal enzyme of PCM
CYP2E1
microsomal enzyme of PCM
CYP2E1
Acetylation Drugs
Sulfonamide
Hydralazine
Isoniazide
Procainamid
Acetylation Drugs
Sulfonamide
Hydralazine
Isoniazide
Procainamid
INH metabolic enzyme
NAT-2 forms DiAcetyl Hydralazine (nontoxic)
Aceful Hydrazine-hepatotoxic metabolite
INH metabolic enzyme
NAT-2 forms DiAcetyl Hydralazine (nontoxic)
Aceful Hydrazine-hepatotoxic metabolite
Methylation Drugs
Histamine->Methy histamine
Nor adrenaline->Adrenaline
Codeine ->Morphine
CYP2D6.
Fluoxetine-inhibits
Tamoxifen-activates
CYP2C9
Warfarin
Phenytoin
Losartan
CYP2C9
Warfarin
Phenytoin
Losartan
Cyp1A2
Activates procarcinogen
Metabolite of Theophylline
Cyp1A2
Activates procarcinogen
Metabolite of Theophylline
CYP2C19
PPI
Omeprazole-excess activation
Not used with Clopidogrel (prodrug activated by CYP2C19
Microsomal enzyme inducers
Griseofulvin
Phenytoin
Rifampicin
Smoking, St. John’s Wort
Carbemezapine
Phenobarbitone
GPRS Cell Phone
Microsomal enzyme inducers
Griseofulvin
Phenytoin
Rifampicin
Smoking, St. John’s Wort
Carbemezapine
Phenobarbitone
GPRS Cell Phone
Microsomal enzyme Inhibitors
Valproate
Ketoconazole
Cimetidine
Ciprofloxacin
Erythromycin
INH
Vit K Can Cause Enzyme Inhibition
Hoffman’s Elimination Eg
ATRACURIUM
Metabolite-LAUDANOSINE-seizures.
Hoffman’s Elimination Eg
ATRACURIUM
Metabolite-LAUDANOSINE-seizures.
High 1st pass metabolism
Propranolol
Salbutamol
Theophylline
Verapamil
Lignocaine
Nitrates except IMN
Zero order kinetics
Warfarin
Alcohol
Aspirin
Tolbutamide
Theophylline
Phenytoin
WAATT Power
Ligand gated receptors
Nm-Na, ca
GABA A - CI
NMDA, AMPA-Na, Ca
5HT3_Na
Ligand gated receptors
Nm-Na, ca
GABA A - CI
NMDA, AMPA-Na, Ca
5HT3_Na
Muscarinic receptors.
M2 and M4-Gi
M1, M3, M5- Gq
Muscarinic receptors.
M2 and M4-Gi
M1, M3, M5- Gq
cAMP GPCR
beta-Gs
Alpha-2-Gi
cAMP GPCR
beta-Gs
Alpha-2-Gi
PLC-IP3+ DAG
Alpha1- Gq
PLC-IP3+ DAG
Alpha1- Gq
ENZYME LINKED Receptors
Insulin-Tyrosine kinase
GH, PRL, Erythropoietin- JAK
Cytoplasmic receptors
Steroid hormones
Vit D
Estrogen
Progesteron
Testosterone
Cytoplasmic receptors
Steroid hormones
Vit D
Estrogen
Progesteron
Testosterone
Nuclear receptor
Thyroid hormone
Inverse agonist of BZD receptor
Beta carboline
Inverse agonist of BZD receptor
Beta carboline
Inverse agonist of H3 receptor
PITOLISANT
Inverse agonist of H3 receptor
PITOLISANT
Inverse agonist of Cannabinoid receptor
RIMONABANT
used for smoking control & obesity
ADR-Severe psychiatric problem- withdrawn
Inverse agonist of Cannabinoid receptor
RIMONABANT
used for smoking control & obesity
ADR-Severe psychiatric problem- withdrawn
Inverse agonist of Cannabinoid receptor
RIMONABANT
used for smoking control & obesity
ADR-Severe psychiatric problem- withdrawn
Physiological Antagonist of Histamine
Adrenaline
Tachyphylaxis means
Rapid tolerance
Eg: Thyramine, Ephedrine
Tachyphylaxis means
Rapid tolerance
Eg: Thyramine, Ephedrine
ADR types
Type A- Augmented Reactions
Type B- Bizarre reactions
Type C- Chronic reactions
Type D - Delayed Reactions
Type E- End of Dose reactions
Type F- Failure of Action
phocomelia by Thalidomide is due to
VGFR antagonism
Warfarin teratogenicity
Fetal Chondrodysplasia punctata
Contradi Syndrome
Nasal hypoplasia
Lithium teratogenicity
Ebstein’s anomaly - Box shaped heart
Tricuspid Atresia
Floppy baby syndrome
Fetal goitre
Lithium teratogenicity
Ebstein’s anomaly - Box shaped heart
Tricuspid Atresia
Floppy baby syndrome
Fetal goitre
Most teratogenic antiepileptic
Sodium Valproate
Most teratogenic antiepileptic
Sodium Valproate
Fetal alcoholic syndrome
Microcephaly
Maxillofacial abnormalities
Movement hyperkinetic
Mental retardation
Myocardial problem (VSD, ASD)
Fetal alcoholic syndrome
Microcephaly
Maxillofacial abnormalities
Movement hyperkinetic
Mental retardation
Myocardial problem (VSD, ASD)
FAS caused by
Thio amide
Methimazole
Carbimazole
Propyl thiouracil
PTV relatively sage
FAS caused by
Thio amide
Methimazole
Carbimazole
Propyl thiouracil
PTV relatively sage
Tetracycline teratogenicity
Discoloration of teeth
Depressed bone growth
Mother- Hepatotoxic
Tetracycline teratogenicity
Discoloration of teeth
Depressed bone growth
Mother- Hepatotoxic
Medical closure of PDA
Indomethain
Ibuprofen
PCM
Indomethacin teratogenicity
Premature closure of ductus arteriosus
Indomethacin teratogenicity
Premature closure of ductus arteriosus
Misoprostol teratogen
Moebius syndrome (6 and 7 CN AbN)
DES teratogen
Female vaginal ca
male-hypospadiasis
Nn ganglionic blockers
Hexamethonium
Trimethaphan
Mecamylamine- smoking control
MAb against beta amyloid in Alzheimer’s disease
Adalumab
Lecanemab
Donanemab
Oximes for OPC poisoning
PRALIDOXIME
OBIDOXIME
DIACETYL MONO OXIME (CNS)
M3 antagonist for intestine and urinary bladder
Darifenacin
Solifenacin
M3 antagonist for intestine and urinary bladder
Darifenacin
Solifenacin
Vesicoselective anticholinergics
OXYBUTYNIN
FLAVOXATE
TOLTERODINE
FESOTERODINE
TROSPIUM CHLORIDE (in Alzheimer’s patients)
MYDRIATIC ANTICHOLNERGICS
Atropine- longest
Homatropine
Cyclopentolate
Tropicamide (MC) Shortest and fastest