What are orphan drugs used for?
Rare diseases; development is low due to low profitability.
What is an orphan receptor?
A receptor with an unknown ligand.
Criteria for essential drugs?
Inexpensive, non-toxic, easily available, efficacious, safe, and single molecule (not FDC).
What are prescription/legend drugs?
Drugs that require a prescription (under Schedule H).
What are spurious drugs?
Drugs that do not produce the expected effect because the drug component is falsified.
What are misbranded drugs?
Drugs with incorrect or missing information on the label.
What are adulterated drugs?
Drugs that contain unwanted additives.
Define rational drug use.
Right drug for right disease & patient; at right dose, duration & route with correct monitoring.
Main mechanism of drug absorption?
Passive diffusion along the concentration gradient.
Where is maximum drug absorption in the GIT?
Small intestine due to large surface area.
Drugs with poor oral absorption?
Large molecules like proteins and -tide/-ase/-mab drugs.
Purpose of enteric coating?
Protects drug from acidic pH of the stomach.
Define bioavailability.
Extent of drug absorption; calculated as AUC oral / AUC IV.
Function of ABC transporters?
Efflux of drugs in intestine, liver, BBB to limit drug exposure or enhance excretion.
Name some p-GP substrates.
Digoxin, Loperamide, Cyclosporine, Clarithromycin, etc.
Name p-GP inducers.
Rifampicin, Phenytoin, Carbamazepine.
What is volume of distribution (Vd)?
Apparent volume in which a drug is distributed; Vd = Dose IV / Initial PC.
Significance of high Vd?
Drug mainly in tissues, not accessible to dialysis.
Drugs with high Vd?
BAD DOC: Benzodiazepines, Amphetamines, Digoxin, Opioids, etc.
What protein binds acidic drugs?
Albumin.
What protein binds basic drugs?
Alpha-1-acid glycoprotein.
Phase I reactions?
Drug inactivation via oxidation; CYP3A4 is most common enzyme.
Phase II reactions?
Make drugs water-soluble; glucuronidation by GT is common.
Drugs metabolized by plasma esterase?
Procaine, Esmolol, Succinylcholine, etc.