Pharm-Fast Review Flashcards
The “-azosin”’s belong to which class of drugs?
Alpha blockers
What is the moa for alpha blockers?
Block a1 receptor on arterioles and venues. Normally, activation of the a1 receptor increases production of DAG and IP3 leading to increased Ca++ intracellularly
What are the major ADEs found with alpha blockers?
Orthostatic hypotension-1st dose,
syncope, sinus-tach, and vertigo
What is phenoxybenzamine’s moa?
Noncompetitive a1 and a2 antagonist
What is phentolamine’s moa?
Competitive a1 and a2 antagonist
The “-olols” belong to which class of drugs?
The Beta Blockers
What is the MOA for the BBs?
Block post synaptic B receptor found on heart and skeletal muscle.
What properties are important concerning the BBs?
Membrane stabilizing activity, ISA, lipid solubility and plasma half life
What ADEs are associated with BB?
CV disturbances ( such as CHF, bradycardia, cold extremities), impotence, sleep disturbances, sedation, asthma
What drugs belong to the alpha2 agonist class?
Clonidine and methyldopa
What’s the MOA for a2 agonists?
Decrease sympathetic outflow by stimulating CNS receptors
What are the ADE’s of clonidine?
Rebound HTN, dry mouth, sedation, bradyarrhythmias
What are methyldopa’s ADEs?
Sedation, ✚ Coombs test; pro-drug converted to α-methyl NE
What two drugs belong to the Post- ganglionic sympathetic terminal blockers drug class?
Reserpine and Guanethidine (discontinued in US)
What’s the MOA for reserpine?
Destroys adrenergic synaptic vesicles, thereby depleting NE and decreasing release
What are the ADEs associated with Reserpine?
Rarely used; depression, sedation, dry mouth, edema, bradycardia, night terrors
What drugs are Ganglionic blockers?
Trimethaphan, mecamylamine, and hexamethonium
What’s the MOA for the Ganglionic blockers?
Compete with Ach for ganglionic nicotinic receptor (Nn) that block the opening of the Na/K channels and thus inhibit post-ganglionic sympathetic neurons
What’s significant about the Ganglionic blockers ADEs?
They have side effects from blocking both sympathetics and parasympathetics
What are the ADEs found with Ganglionic blockers?
Postural hypotension, tachycardia, arrhythmias, blurred vision, double vision, asthma, dry mouth, constipation, paralytic ileus, urinary retention, impotence, drowsiness, seizures, hallucinations, tremors, and confusion
What drugs belong to the Ca++ channel blockers class?
Drugs ending in “-pine” and Diltiazem and Verapamil
What are the “pines” MOA?
Block L-type Ca++ channels in smooth muscle
What are Diltiazem and Verapamil’s MOA?
Block L-type Ca++ channels in CARDIAC & smooth muscle
What ADEs are associated with the CCBs?
Constipation, edema, headache, bradycardia, GI disturbancies, dizziness, AV block, tachycardia (nifedipine)
What two drugs act directly through NO?
Hydralazine and nitroprusside
What is the MOA for hydrazine and nitroprusside?
Release endothelial NO, which stimulates guanylate cyclase which increases cGMP
What are the side effects associated with hydralazine
Reversible lupus erythematosus- like syndrome, edema, arteriolar dilation
What are the ADEs associated with Nitroprusside?
Used for hypertensive emergencies. ADE=arteriolar and venous dilation, cyanide poisoning
What are the drugs opening K+ channels?
Minoxidil and Diazoxide
What is the MOA for the drugs opening K+ channels?
Open K+ channels which leads to hyperpolarization of VSM
What are the ADEs for MInoxidil?
For severe HTN; hirsutism, pericardial effusion, edema
What are the ADEs for Diazoxide?
For HT emergencies; hyperglycemia
What drug is a D1 agonists?
Fenoldopam
What’s the MOA of fenoldopam?
Vasodilates renal vessels
What’s fenoldopam used for?
For HT emergencies
What drugs are the ACEi?
The “-Prils”
What are the ACEi MOA?
Blocks formation of Ang II which leads to a decrease in aldosterone
What side effects are associated with ACEi?
Cough, hyperkalemia, angioedema, renal damage in pre-existing renal disease, contraindicated in pregnancy (fetal damage)
Which drugs are the ARBs?
The “Sartans”
What’s is the MOA for the ARBs?
They block Ang II at AT1 receptor; which leads to a decrease in aldosterone
What side effects are associated with the ARBs?
Renal damage in pre-existing renal disease, hyperkalemia; contraindicated in pregnancy (fetal damage)
What drug is a renal inhibitor?
Aliskerin
What is the MOA for Aliskerin?
It decreases Ang I and therefore Ang II and aldosterone
What ADE is found with Aliskerin?
Hyperkalemia
What Thiazide do we still need to remember?
HCTZ
What does HCTZ do?
Inhibits Na+/Cl- transporter
What side effects are associated with HCTZ?
Useful in mild HTN; Causes
Decreases in K+, Mg2+, Na+ and causes
Increases in Ca2+, uric acid, glucose, LDL cholesterol, triglycerides
Which Loop diuretic do we need to know?
Furosemide
What’s Furosemides MOA?
Inhibit Na+/K+/2Cl- transporter
What ADEs are associated with Furosemide?
Useful in moderate-severe HTN;
Cause a decrease in K+, Mg2+, Ca2+, Na+ And an increase in uric acid, glucose, LDL cholesterol, triglycerides
What drug is an Aldosterone antagonists?
Spironolactone
What’s spironolactone’s MOA?
Aldosterone antagonist in DCT
What ADEs are associated with spironolactone?
Hyperkalemia, metabolic acidosis, gynecomastia; safe for use in pregnancy
What drugs are indicated in pregnancy for the Rx of HTN?
α-methyldopa and Hydralazine
What drugs are contraindicated during pregnancy for HTN Rx?
ACEIs, ARBs
What drugs are indicated for diabetes for the Rx of HTN?
ACEIs, ARBs
What drugs are contraindicated in diabetics for the Rx of HTN?
BB (high doses)
Note:Add-on use in low doses; diuretics also good 2nd line agents
What drugs are indicated for the Rx of HTN in heart failure?
ACEIs
What drugs are contraindicated for the Rx of HTN in heart failure?
BB (high doses); verapamil, diltiazem
Note:Add-on use with low dose BBs, ARBs, diuretics (all classes); select CCBs (amlodipine, felodipine)
What drugs are indicated for the Rx of HTN in COPD/ asthma?
CCBs
What drugs are contraindicated for the Rx of HTN in COPD/asthma?
BBs (non-selective; high dose).
ACEIs NOT recommended owing to chronic cough
What drugs are indicated for the Rx of HTN in CKD?
ACEIs, ARBs
What drugs are indicated for the Rx of HTN in BPH?
α-blockers
What drugs are contraindicated for Rx of HTN in individuals with severe depression?
BBs, reserpine, α-methyldopa
What drugs are indicated for the Rx of HTN Post-MI?
BBs, spironolactone, cardiac CCBs.
ACEIs also acceptable
What drugs are indicated for Prophylaxis of recurrent stroke?
Diuretics, ACEIs
