Module 6: Hypertension Pharmacology Flashcards
Explain the principles of drug management of dyslipidemia.
a
Discuss the mechanism of action and effects of major classes of antihyperlipidemics.
a
List the major side-effects of the above medications.
a
blood pressure is linked to several cardiovascular parameters such as
CO, fluid volume, TPR
Antihypertensive therapy can be divided into what 5 categories list their target
- Drugs that target sympathetic activity
- > Target: TPR and HR - Vasodilators
- > Target: TPR - Calcium channel blockers
- > Target: CO and TPR - Angiotensin Converting Enzyme Inhibitors (ACEIs) and Angiotensin Receptor
Blockers (ARBs)
-> Target: Vascular resistance and fluid volume - Diuretics
- > Target: Fluid volume
What are G proteins
- Membrane-spanning proteins
- Cytoplasmic tail linked to G protein, a 3-part transducer molecule
What happens When G proteins are activated,
- open ion channels in the membrane
2. alter enzyme activity on the cytoplasmic side of the membrane
Gs is coupled to what receptors
Beta 1, beta 2, dopamine 1
Gi is coupled to what receptors
Alpha 1, muscarinic 2
Discuss the a) mechanism b) example c) uses d) notes of Alpha 2 receptor agonist
a) Mechanism: stimulates alpha 2 receptors which decrease sympathetic outflow and thus decreasing total peripheral resistance (which decreases blood pressure) and heart rate (which decreases cardiac output and eventually decrease blood pressure).
b) Example: Clonidine and methyldopa.
c) Uses: mild to moderate hypertension.
d) Notes: These drugs may have interactions with other classes of medications. Methyldopa is considered a good option to treat hypertension during pregnancy.
Discuss the a) mechanism b) example c) uses d) notes of Alpha 1 receptor antagonist
a) Mechanism: Alpha 1 receptor blocker which results in smooth muscle relaxation and a decrease in vascular resistance.
b) Example: Doxazosin (and any drug that has the surname -zosin)
c) Uses: Hypertension
d) Notes: May result on orthostatic hypotension. They are a favored class of drugs because they result in a desired lipid profile (particularly increase in high density lipoprotein and decrease in low density lipoprotein).
Discuss the a) mechanism b) example c) uses d) notes of Beta Blockers
a) Mechanism: When beta receptors are blocked:
- > CO dec so this leads to dec in BP,
- > Dec the release of Renin from the kidney (which if you recall can stimulate the conversion of Angiotensin I to Angiotensin II) and eventually aldosterone.
b) Example: Propranolol (and any drug that has the surname –olol). The pharmacology of beta blockers is interesting because some of these beta blockers can block both Beta 1 and Beta 2 receptors (propranolol) or only beta 1 receptors (metoprolol).
c) Uses: this class of medications if favored for treating hypertension particularly in patients with concomitant heart disease such as a previous myocardial infarction, angina pectoris and heart failure.
d) Notes: These drugs may result in bradycardia. Unlike alpha 1 receptor blockers, the beta blockers can alter lipid profile (particularly increasing low density lipoprotein and triglycerides).
Discuss the a) mechanism b) example c) uses d) notes of Vasodilators
a) Mechanism: one particular class allows for the opening of the potassium channels resulting in hyperpolarization of smooth muscles and eventually smooth muscle relaxation and subsequent vasodilation.
b) Example: Minoxidil and diazoxide.
c) Uses: severe hypertension.
d) Notes: Minoxidil has an interesting side effect, it can trigger hypertrichosis (hair growth). Diazoxide on the other hand can decrease insulin resistance.
Discuss the a) 3 diff types b) mechanism c) uses d) notes of Calcium Channel Blockers
a) These are available in three types:
- Diphenylalkylamines: an example would be verapamil.
- Benzothiazepines: an example would be diltiazem.
- Dihydropyridines: an example would be nifidipine (and drug that has the surname –dipine).
b) Mechanism: these drugs can block the L-type calcium channels in both cardiac muscle and blood vessels such as verapamil and diltiazem. Dihydropyridines have more affinity towards vascular calcium channels.
c) Uses: Hypertension but they can be used to treat other cardiovascular diseases.
d) Notes: they can cause flushing and headache because of the vasodilation. Another interesting side effect is the gingival hyperplasia.
Discuss the a) mechanism b) example c) uses d) notes of Renin Inhibitors
a) Mechanism: see above.
b) Example: Aliskiren.
c) Uses: hypertension.
d) Notes: Aliskiren have multiple drugs interactions and it can cause angioedema.
Discuss the a) mechanism b) example c) uses d) notes of ACEIs
a) Mechanism: See above.
b) Example: Captopril and any drug that has the surname –pril.
c) Uses: mild to moderate hypertension.
d) Notes: can cause angioedema, dry cough and hyperkalemia.
Discuss the a) mechanism b) example c) uses d) notes of ARBs
a) Mechanism: See above.
b) Example: Losartan and any drug that the surname –sartan.
c) Uses: mild to moderate hypertension.
d) Notes: same as ACEIs although the ARBs are the ideal alternative when patients develop the dry cough while using ACEIs.
Discuss the a) mechanism b) example c) uses d) notes of Aldosterone Receptor Antagonist
a) Mechanism: See above.
b) Example: Spironolactone.
c) Uses: hypertension and any condition that increases aldosterone.
d) Notes: may cause hyperkalemia and has an antiandrogen effect.
Discuss the a) mechanism b) example c) uses d) notes of Aldosterone Receptor Antagonist
a) Mechanism: See above.
b) Example: Spironolactone.
c) Uses: hypertension and any condition that increases aldosterone.
d) Notes: may cause hyperkalemia and has an antiandrogen effect.
What are the 2 classes that are used in treating hypertension.
Loop and Thiazide Diuretics
Discuss the a) mechanism b) example c) uses d) notes of Loop Diuretics
a) Mechanism: these medications can inhibit a cotransport of Na+/K+/2Cl- in the luminal membrane of the ascending loop on Henle in the nephron system. This will result in decrease reabsorption of these ions so they will promote diuresis.
b) Example: Furosemide, Torsemide, and Ethacrynic Acid.
c) Uses: Hypertension, a state of pulmonary edema or even peripheral edema triggered by heart failure.
d) Notes: These drugs (Ethacrynic acid is the exception) contain sulfa products to which many people have hypersensitivity. Patients taking these drugs may experience hypocalcemia, hypomagnesemia, hyperuricemia and volume depletion. They may also cause ototoxicity.
Discuss the a) mechanism b) example c) uses d) notes of Thiazide Diuretics
a) Mechanism: these medications inhibit the Na+/Cl- Thiazides work mainly in the cortical region of the ascending loop of Henle and the distal convoluted tubule.
b) Example: Indapamide, Chlorothiazide and hydrochlorothiazide. These drugs will increase the excretion of sodium and chloride, loss of potassium, loss of magnesium and impair the kidney’s ability to excrete calcium.
c) Uses: Hypertension and heart failure.
d) Notes: Similar to loop diuretics, they may trigger hypersensitivity because of the sulfa group. They also cause depletion of potassium, hyperuricemia, hypercalcemia, hyperglycemia and hyperlipidemia. Indapamide doesn’t affect lipid profile.
Explain the principles of drug management of dyslipidemia.
a
Discuss the mechanism of action and effects of major classes of antihyperlipidemics.
a
List the major side-effects of the above medications.
a
