Pharmacy Foundations Flashcards
Muscarinic receptor
Substrate acetylcholine
Agonist: paraympathetic ANS (wet) (pilocarpine, bethanechol)
Antagonist: sympathetic (dry) (atropine, oxybutynin)
Nicotinic receptor
Substrate: acetylcholine
Agonist: increase HR and BP (nicotine)
Antagonists: neuromuscular blockade (rocuronium etc)
Alpha-1 receptor
Substrate; epinephrine, norepinephrine
Mainly peripheral
Agonist: vasoconstriciton of smooth muscles and increased BP (phenylephrine, dopamine)
Antagonist: vasodilation of smooth muscles and decreased BP (doxazosin, carvedilol, phentolamine)
Alpha-2 receptor
Substrate; epinephrine, norepinephrine
Mainly central and brain
Agonist: inhibits release of Epi and NE, decreased BP and HR (clonidine, brimonidine)
Antagonist: increased BP and HR (ergot alkaloids, yohimbine)
Beta-1 receptor
Substrate; epinephrine, norepinephrine
Mainly heart
Agonist: increased contractility, CO, HR (dobutamine, isoproterenol, dopamine)
Antagonist: decreased CO and HR (metoprolol, propranolol, carvedilol)
Beta-2 receptor
Substrate: epinephrine
Mainly in lungs
Agonist: bronchodilator (albuterol, terbutaline, isoproterenol)
Antagonist: bronchoconstriction (propranolol, carvedilol)
Dopamine receptor
Substrate: dopamine
Agonist: renal, cardiac, and CNS effects (levodopa, pramipexole)
Antagonist: renal, cardiac, and CNS effects (haloperidol, metoclopermide)
Serotonin receptor
Substrate: serotonin
Agonist: platelet, GI, psychiatric (triptans)
Antagonist: platelet, GI, psychiatric (ondansetron, quetiapine)
Acetylcholinesterase
Breaks down acetylcholine
Inhibitors: donepezil, rivastigmine, galantamine
Results in increased ACh to treat Alzheimer’s
Angiotensin-converting enzyme
Converts angiotensin I to II that controls vasoconstriction
Inhibitors: lisinopril, ramipril
Resulting in decreased vasoconstriction and aldosterone secretion to treat hypertension, HF, and kidney disease
Catechol-O-methyltransferase
Breaks down levodopa
Inhibitor: entacapone
Blocks peripheral breakdown resulting in better duraiton of levodopa to treat Parkinson’s
Cyclooxygenase
Converst arachidonic acid to prostaglandins to cause inflammation, and thromboxane A2 to cause platelet aggregation
Inhibitors: aspirin, ibuprofen
Results in decreased inflammation, and platelet aggregation
Monoamine oxidase
Breaks down catecholamines (DA, NE, 5-HT)
Inhibitors: phenelzine, tranylcypromine, isocarboxazid, selegiline, rasagiline, methylene blue, linezolid
Results in increased catecholamine levels to treat depression
Overdose: hypertensive crisis, serotonin syndrome
Phosphodiesterase
Breaks down cGMP, which is a smooth muscle relaxant
Inhibitors (5): sildenafil, tadalafil
Competitively binds to cGMP active site on the PDE-5 enzyme resulting in smooth muscle relaxation to treat erectile dysfunction
Vitamin K epoxide reductase
Converts vitK to the active form to create clotting factors
Inhibitor: warfarin
Results in less clotting factors being produced such as II, VII, IX, X for blood clot prevention
Xanthine oxidase
Breaks down hypoxanthine and xanthine to uric acid
Inhibitor: allopurinol
Results in decreased uric acid production to treat gout
Neutral functional groups
Alcohol primary group, ketone, aldehyde, amide, nitrate, nitro, aromatic benzene ring, urea, carbonate, carbamate, ether, thioether
Acidic functional groups
Carboxyl, phenol, imide, sulfonamide
Basic functional groups
Amine primary group, amine tertiary group, imine, amidine
Essential drug structures
Amoxicillin, ceftriaxone, ertapenem, aztreonam, gentamicin, sulfamethoxazole, aspirin, ibuprofen, amphetamine, levothyroxine, amiodarone, fenofibrate, amitriptyline, chlorpromazine
Common prodrugs
Capecitabine; fluorouracil
Clopidogrel; metabolites active
Codeine; morphine
Colistimethate; colistin
Famciclovir; penciclovir
Fosphenytoin; phenytoin
Isavuconazonium sulfate; isavuconazole
Levodopa; dopamine
Lisdexamfetamine; dextroamphetamine
Prednisone; prednisolone
Primidone; phenobarbital
Tramadol; metabolites active
Valacyclovir; acyclovir
Valganciclovir; ganciclovir
Common CYP inhibitors
GPACMAN
Grapefruit juice
Protease inhibitors, especially ritonavir
Azole antifungals
Cyclosporine, cobiscistat
Macrolides, except azithromycin
Amiodarone, dronedarone
Non-DHP CCB
Common CYP inducers
PS PORCS
Phenytoin
Smoking
Phenobarbital
Oxcarbazepine
Rifampin, rifabutin, rifapentine
Carbamazepine
St. John’s Wort
Common p-gp substrates, inhibitors, inducers
Substrates: anticoagulants (esp riva and api), cardiovascular (esp digoxin, verapamil, diltiazem), immunosuppressants (esp cyclosporine, tacrolimus), HCV drugs, and colchicine
Inducers: same as CYP inducers plus dexamethasone, and tipranavir
Inhibitors: Anti-infectives, cardiovascular drugs (esp amiodarone, diltiazem, verapamil), HIV drugs (esp cobiscistat, ritonavir), cyclosporine
Common CYP substrates
3A4: Analgesics, anticoagulants, immunosuppressants, statins, HIV (esp NNRTI), PDE-5 inhibitors, ethinyl estradiol
1A2: theophylline, warfarin
2C8: amiodarone, pioglitazone, repaglinide
2C9: warfarin
2C19; clopidegrel
2D6: analgesics, antipsychotics, antidepressants, tamoxifen