Term
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Definition
alpha-2 agonist
MOA: stimulate α2 receptors (Centrally)
Indications: ADHD, Pain management (epidurals) Methyldopa is used in pregnancy!
Adverse: sudden stoppage- rebound hypertension (nervousness, tachycardia, sweating); orthostatic hypotension (minimal), dizziness, bradycardia, fatigue/sedation, dry mouth. |
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Term
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Definition
alpha-1 antagonist
MOA: prevents activation of a-1 receptors peripherally
Indications: Hypertension; BPH
Adverse: First-dose othostatic hypotension (give at night); syncope, especially with first dose; reflex tachycardia; impotence/inhibition of ejaculation |
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Term
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Definition
alpha/beta blocker
MOA: alpha-1 and beta blockade
Indications: labetalol used exclusively in pregnancy; hypertension; heart failure; dysrhythmias; angina; less common-migraines, anxiety
Adverse: weakness, diarrhea, sexual dysfunction; bradycardia; rebound hypertension; heart failure/pulmonary edema
Contraindications: non-selective beta blockers-astma/COPD?; severe bradycardia; uncompensated heart failure |
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Term
| metoprolol tartrate/succinate |
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Definition
beta-1 specific blocker
MOA: beta-1 specific blocker
Indications: hypertension; heartt failure; dysrhythmias; angina; less common-migraines, anxiety
Adverse: weakness, diarrhea, sexual dysfunction; bradycardia; rebound hypertension; heart failure/pulmonary edema
Contraindications: non-selective beta blockers-astma/COPD?; severe bradycardia; uncompensated heart failure |
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Term
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Definition
ACE inhibitor
MOA: prevents ACE from converting angiotensin I to angiotensin II; decreased aldosterone release; decreased vasoconstriction; decreased preload and afterload.
Pharmacokinetics: Enalapril is a prodrug (called enalaprilat when IV), Lisinopril is NOT a prodrug, you will see this a LOT!
Indications: hypertenion (especially in diabetes, CKD); heart failure; post MI (prevent remodeling)
Adverse: Hyperkalemia; chronic, non-productive cough; initial increase in serum creatinine-may require dose reduction-watch acute renal failure (ARF) |
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Term
| ACE inhibitor adverse effects |
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Definition
Angioedema
-Up to 5 times higher incidence in people of african descent
Boxed Warning:
-Drugs that work on the RAAS can cause injury and death to a developing fetus
-Not recommended in pregnancy (class C in 1st trimester and class D in 2nd/3rd trimester) |
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Term
| ACE inhibitor drug/drug interactions |
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Definition
-Can cause hyperkalemia, especially upon initiation. Take consideration of other drugs that can cause elevated potassium
--Case reports of sudden death in geriatric patients who were prescribe ACE-Inhibitors and an antiobiotic- sulfamethoxazole-trimethoprim (Bactrim DS®)
-Lithium can accumulate, potential for toxicity
-Be careful with diuretics
-NSAIDS/ASA (aspirin)
-COX inhibitors
--celecoxib (Celebrex)
-CONTRAINDICATION
--Renal Artery Stenosis |
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Term
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Definition
Angiotensin II receptor blocker
MOA: blocks binding of angiotensin II
Pharmacokinetics: oral route only
Indications: Hypertension (diabetes and CKD); Adjunct in Heart Failure; Post M.I.
Adverse: Hyperkalemia (less than ACE-I); BOXED WARNING: Fetal Harm RAAS Drugs; some angioedema- unknown how it affects bradykinin |
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Term
| angiotensin II receptor blocker drug/drug interactions |
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Definition
-DRUG DRUG INTERACTIONS
--Potassium sparing medications
--Lithium
--NSAIDS
-CONTRAINDICATIONS
--Renal Artery Stenosis |
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Term
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Definition
renin inhibitor
MOA: direct renin inhibitor, resulting in blockade of the conversion of angiotensinogen to angiotensin I
pharmacokinetics: Poor absorption (worse w/meals); Onset: 2 weeks for full antihypertensive effect
Indications: Hypertension, still fairly new class so its trying to find its way
Adverse: Hyperkalemia; SJS and TEN have been reported; BOXED Warning: Drugs that work on the RAAS can cause injury and death to a developing fetus; angioedema- unknown how it affects bradykinin
Drug/Drug: NSAIDS, COX inhibitors; other potassium sparing drugs |
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Term
| calcium channel blocker activation site |
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Definition
Vascular Smooth Muscle
-peripheral arteries and arteries of the HEART
-no effect on veins
Heart
-Myocardium- positive inotropic effect
-SA Node- Pacemaker- control heart RATE
-AV Node- coordinating contraction |
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Term
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Definition
Non-DHP (dyhydropyridines) calcium channel blocker
MOA: prevents Ca influx into vascular smooth muscle; dilates peripheral and cardiac vessels; prevent Ca influx into cardiac tissue
Indications:Hypertension; Arrhythmias ; Angina; off label migraine prevention
Adverse: Headache, dizziness, flushed skin; peripheral edema; constipation (verapamil); bradycardia; ventricular Arrhythmias |
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Term
| Non-DHP calcium channel blocker cautions |
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Definition
-Heart Block (impaired conduction of electrical signals throughout conduction pathway of the heart)
-Heart failure
-Hypotension/Bradycardia
DRUG DRUG INTERACTIONS
-These are CYP3A4 inhibitors!
-NO GRAPE FRUIT JUICE |
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Term
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Definition
DHP calcium channel blocker
MOA: prevents Ca influx into vascular smooth muscle; Dilates peripheral and cardiac vessels
Pharmacokinetics: nifedipine-used in pregnancy!
Indications: Hypertension; Angina; Delay premature Labor; off label Raynauds Disease; off label Migraine prevention
Adverse: Headache, dizziness, flushed skin; profound hypotension-reflex tachycardia (baroreceptor reflex); peripheral edema |
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Term
| DHP calcium channel blocker cautions |
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Definition
-Heart Block (impaired conduction of electrical signals throughout conduction pathway of the heart)
-Heart failure
-Hypotension/Bradycardia
DRUG DRUG INTERACTIONS
-These are CYP3A4 substrates!
-NO GRAPEFRUIT JUICE |
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Term
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Definition
methyldopa
labetalol
nifedipine |
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Term
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Definition
vasodilators
MOA: act directly on arteriolar and/or venous smooth muscle; artery- afterload; vein- preload
Pharmacokinetics: Sodium Nitroprusside-exremely short half life (10 minutes); metabolites include cyanide
Indications: acutely for heart failure; hypertension (urgency/emergency; African decent)
Adverse: fluid retention; hyralazine-induced lupus-like syndrome (book says it can actually cause systemic lupus erythematosus); reflex tachycardia |
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Term
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Definition
vasodilators
MOA: act directly on arteriolar and/or venous smooth muscle; artery- afterload; vein- preload
Pharmacokinetics: Sodium Nitroprusside-exremely short half life (10 minutes); metabolites include cyanide
Indications: Hypertensive Emergency-Titratable drip; Usable in acute decompensated heart failure
Adverse: severe hypotension; cyanide toxicity (renal failure, long period of use); drug must be protected from light (light can break down drug)
-CYANIDE ANTIDOTE KITS: sodium nitrite and sodium thiosulfate (can also see cyanide poisoningi from smoke inhalation from fires) |
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Term
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Definition
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Term
| hydrochlorothiazide (HCTZ) |
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Definition
diuretic-thiazides
MOA: work on the distal convoluted tubule in the kidney, inhibiting Na, Mg, K, and Cl resorption.
Indications: hypertension, heart failure, edema.
Adverse: hypokalemia, hypomagnesemia, hyponatremia, hypocholeremia
-Hypercalcemia; Hyperlipidemia; Hyperglycemia,; Hyperuricemia
-Frequent urination
-photosensitivity |
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Term
| Thiazide contraindiations |
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Definition
Sulfa allergy- derived from sulfonamide Abx
caution in liver disease
Severe renal failure (CrCl<30ml/min) |
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Term
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Definition
Non black-thiazide; CCB; ACEI/ARB
Black-thiazide; CCB
CKD-ACE/ARB |
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Term
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Definition
HMG CoA reductase inhibitor
MOA; competitively inhibit the formation of cholesterol in hepatocytes; Up-regulate LDL receptors, leading to increased LDL uptake into hepatocytes
Pharmacokinetics: CYP3A4 metabolism; give at night!
Indications: LDL levels (1st line therapy, most potent LDL reducers); Post MI, Post stroke
Adverse: Headache, GI issues; FDA Warning: Myopathy -> Rhabdomyolysis ; FDA Warning: Memory loss, confusion; FDA Warning: increased blood glucose, HgbA1C; elevated liver enzymes; Recommend baseline LFTS, and potentially CK |
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Term
| HMB CoA reductase inhibitor contraindications |
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Definition
CATEGORY X IN PREGNANCY!
DRUG DRUG INTERACTIONS
-Oral Anticoagulants (warfarin)
-CYP3A4 Metabolism
-Grapefruit Juice can severely increase the statin concentration (risk for rhabdomyolysis), Macrolide Antibiotics (Erythromycin), Antifungals and antivirals
-Other cholesterol Meds
-Caution in gemfibrozil (fibrate), usually avoid
**FDA pretty particular with simvastatin dosing
-New patients are no longer allowed to use 80 mg dose
-20 mg max if on amlodipine/amiodarone/ranolizine
-10 mg max if on verapamil/diltiaze |
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Term
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Definition
fibrates
MOA: Bind to PPARα, causing many changes in liver and muscle cells; Increased HDL synthesis; Decreased inhibiton of triglyceride uptake by the liver
Indications: elevated TGs; raises HDL
Adverse: Headache, GI issues (N/D); Blurred vision; rarely Myopathy; elevated liver enzymes; increased risk for gallstones; prolonged prothrombin time (clotting issues) |
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Term
| fibrate contraindications |
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Definition
-Severe kidney disease, liver disease, gallbladder disease
DRUG DRUG INTERACTIONS
-Oral Anticoagulants (warfarin)
-Other cholesterol Meds
-Caution in gemfibrozil with statins (generally avoided, rhabdomyolysis risk) |
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Term
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Definition
bile acid sequestrants
MOA: Insoluble polymers that bind bile acids in the gut
Indications: Add on for LDL reduction; Off label for diarrhea
Adverse: Constipation; Heartburn, nausea, belching, bloating; These adverse effects tend to disappear over time
DRUG DRUG INTERACTIONS: Based on timing of administration; Take drugs 1 hour before or 4 to 6 hours after use |
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Term
| nicotinic acid/niacin/vitamin B3 |
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Definition
niacin
MOA :Unknown-Believed to inhibit lipolysis in adipose tissue, decrease esterification of TG in liver, and increase lipoprotein lipase
Pharmacokinetics: Lipid-lowering properties require much higher doses than when used as a vitamin
Indications: Can increase HDL; lower LDL and TGs!
Adverse: elevated liver enzymes (extended release products); pruritus; FLUSHING (common); NSAIDS/ASA can be taken 30 minutes prior; Gradually taper up doses; Increase in uric acid levels; Increase in blood glucose |
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Term
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Definition
-peptic ulcer disease, hepatic disease, gout, hemorrhage
***DRUG DRUG INTERACTIONS
-can have moderate interaction with statins
-slight risk increase for myopathy |
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Term
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Definition
cholesterol absorption inhibitor
MOA: Inhibits absorption of cholesterol and related sterols from the small intestine
Indications: Can increase HDL, lower LDL and TG; typically as an add on with a statin; (Vytorin ezetimibe/simvastatin); One of newest classes, trying to find a spot in regimens
Adverse:Myopathy (less than statins); elevated LFTs; GI issues (Diarrhea) |
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Term
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Definition
Used as an antispasmodic, antihypertensive, antiplatelet, lipid reducer
Adverse effects: dermatitis, vomiting, diarrhea, flatulence, antiplatelet activity
Possible interactions with warfarin, diazepam
May enhance bleeding when taken with NSAIDs |
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Term
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Definition
Fish oil/flax products
Used to reduce cholesterol
May cause rash, belching, allergic reactions
Potential interactions with anticoagulant drugs |
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Term
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Definition
60% to 70% of sodium and water is returned to bloodstream by the proximal tubule
20% to 25% of all sodium is reabsorbed into the bloodstream in the ascending loop of Henle
5% to 10% is reabsorbed in the distal tubules
3% is reabsorbed in collecting ducts
If water is not absorbed, it is excreted as urine |
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Term
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Definition
osmotics
MOA: simple six carbon sugar that undergoes minimal reabsorption in the nephron. Potent effects in the proximal tubule and descending Loop of Henle
Indications: prevention of renal failure; reduction of intracranial pressure (cerebral edema); NOT used for edema (doesn't pull sodium)
Adverse: Pulmonary Edema (ICF vs. ECF); can form a precipatant. Must be filtered and typically warmed |
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Term
| hydrochlorothiazide/metolazone |
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Definition
thiazides
MOA: work on the distal convoluted tubule in the kidney, inhibiting Na, Mg, K, and Cl resorption
Indications: Hypertension; Heart Failure; Edema
Adverse:
-Hypokalemia, Hypomagnesemia, Hyponatremia, Hypochloremia
-Hypercalcemia, Hyperlipidemia, Hyperglycemia, Hyperuricemia
Frequent urination!; Photosensitivity; Dizziness,lightheadedness, weakness |
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Term
| thiazide contraindications |
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Definition
Sulfa allergy-derived from sulfonamide Abx
Caution in liver disease
Severe renal failure (CrCl<30ml/min)
metolazone being the exception |
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Term
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Definition
loop diuretics
MOA: hypertension; edema due to heart failure
Adverse:Hypokalemia, Hypomagnesemia, hyponatremia, Hypocalcemia; Hyperlipidemia, Hyperglycemia, Hyperuricemia; Frequent urination!; Ototoxicity (rare), tinnitus; Photosensitivity; Dizziness,lightheadedness, weakness |
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Term
| loop diuretics contraindications |
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Definition
-Sulfa allergy- derived from sulfonamide Abx
exception being ethacrynic acid
-Severe electrolyte loss
***DRUG DRUG INTERACTION
-Lithium toxicity
-aminoglycosides (ototoxicity)
-NSAIDS can diminish response |
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Term
| triameterene/spironolactone |
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Definition
potassium sparing diuretics
MOA: Inhibit exchange of Na+ and K+ in the distal tubule and collecting ducts -Spironolactine inhibits aldosterone binding
Indications: Heart Failure (spironolactone); Edema; Ascites; Hypertension; Hypokalemia
Adverse: Spironolactone structure similar to steroid
gynecomastia, hirsutism, deepening of the voice; Hyperkalemia (muscle cramps, arrhythmias); Frequent urination!; Dizziness,lightheadedness, weakness |
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Term
| potassium sparing diuretic contraindications |
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Definition
-Hyperkalemia
***DRUG DRUG INTERACTIONS
-Lithium toxicity
-Other potassium sparing drugs
-NSAIDS can diminish response |
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