Pharmacology Flashcards
Which drug characteristic makes a drug more likely to enter a cell through a protein channel?
Water soluble drug
inhibitors and agonists of the drugs (3)
allosteric agonis
allosteric inhibitor
competitive inhibitor
Characteristics of hydrophilic drugs (4)
usually polar
aqueous diffusion
requires pores or transporters
usually don’t croos the Blood Brain Barrier (BBB) and Blood Uterine Barrier (BUB)
Characteristics of lipophilic drugs (4)
Usually non polar
Lipid diffusion
Often cross barriers
usually cross the BBB and BUB
What is the Pka?
Is the ratio of the drug will be 50% protonated and 50% Nonprotaned
Ex: aspirin pka = 3.8
PH = 3.8 →aspirin 50% protonated and 50% nonprotonated
Acid Pka and Basic Pka
Acid drug →The more acid, less protonated
Basic drug→ The more acid, more protonated
Base protonated –> more soluble
Acid protonated –> less soluble
What is volume of distribution (Vd)
Vd = amount of drug in the body
Concentation in the blood
Phases of metabolism of drugs
phase 1: makes the drug more polar (CYP 450)
phase 2:makes the drug more hydrophilic adding specifics groups
Phase 3: Prepare the drug for excretion
Factors that affecting drup metabolism (6)
Genetic differences between cytochrome P450
Competitive inhibiton of cytochrome P450
Inhibition of cytochrome P450
induction of cytochrome P450
Inhibitors of P-glycoprotein (phase 3)
blood flow
Inhibitors of CYP450 (5)
Amiodarone
Fluconazole
Cimetidine
Ritonavir
Grapefruit juice
Suicide inhibitors of CYP450
Spirolactone
Ethinylestradiol
Allopurinol
Propylthiouracil
Secobarbital
Inducers of CYP450 (5)
Carbamazepine
Phenobarbital
Phenytoin
Ethanol
St. John’s Wort
Action of P-glycoprotein…
Transport protein that moves drugs from cells into intestinal lumen
Inhibitors of P-glycoprotein (2)
Verapamil
Greap Fruit
Substrates P-Glycoprotein (2)
cyclosporine
Digoxin