Drugs #2

Question 0

Aldosterone

Answer 0

Synthesis catalyzed by angiotensin II. Binds to mineralocorticoid receptor (a nuclear receptor) which increases the expression of Na/K/ATPase, Na/proton antiporter, and Na channels. This occurs in the collecting duct.

Question 1

Mannitol

Answer 1

An osmotic diuretic that resembles glucose but cannot be absorbed in the proximal tubule, or any part of the nephron. Leads to a higher solute concentration in the lumen driving water flow into it, eventually leading to increased water excretion. They reduce the passive reabsorption of water. Used in acute renal failure to keep fluid flowing in the nephrons, and for emergency treatment of intracranial or intraocular pressure. Not useful for control of blood pressure.

Question 2

Desmopressin

Answer 2

Analogue of vasopressin. Used in the treatment of neurogenic diabetes insipidus.

Question 3

Vasopressin

Answer 3

Binds to V2 receptor on basolateral membrane. This increases cAMP levels, which leads to insertion of aquaporins into the apical membrane of the collecting duct.

Question 4

Thiazides

Answer 4

Block Na/Cl cotransporters in the distal tubule. Less powerful than loop diuretics (ceiling effect). Used as antihypertensives and treat cardiac insufficiency.

Question 5

Loop diuretics

Answer 5

Loop diuretics block Na/K/2Cl cotransporter. Bumetanide, furosemide, ethacrynic acid. Used to treat salt and water overload (cardiac insufficiency and pulmonary edema). Anti hypertensives, but thiazides are preferred if good renal function.

Question 6

Spironolactone

Answer 6

Competitive antagonist of aldosterone.

Question 7

Renin inhibitors

Answer 7

Aliskerin.

Question 8

Captopril

Answer 8

ACE inhibitor. Result is decreased blood pressure due to less angiotensin II and more bradykinin (ACE degrades bradykinin), which is a vasodilator. Carboxy terminal of substrate has a bit of a link to interact with a charged group, so Captopril has a proline.

Question 9

Angiotensin II receptor antagonist (AT1 subtype)

Answer 9

Sartans; e.g. Losartan.

Question 10

Amiloride and triamterene

Answer 10

Blocks Na/Cl symporter in the collecting duct. Potassium sparing.

Question 11

Acetazolamide

Answer 11

Carbonic anhydrase inhibitor. Not used as a diuretic. Used to treat glaucoma. Deplete extracellular bicarbonate and causes metabolic acidosis.

Question 12

Diuretics are used to treat:

Answer 12

Hypertension, cardiac insufficiency (heart failure), renal failure, and pulmonary edema.

Question 13

Carazolol

Answer 13

Inverse agonist of beta 2 adrenergic receptors.

Question 14

Phosphodiesterase inhibitors

Answer 14

Methyl xanthines: resemble a nucleotide. Caffeine, theophylline (treats asthma), theobromine (weak).

Question 15

Forskolin

Answer 15

Activates adenylyl cyclase.

Question 16

Norepinephrine

Answer 16

Increased heart rate and blood pressure. Peripheral vasoconstriction.

Question 17

Epinephrine

Answer 17

Increased heart rate and blood pressure. Peripheral vasoconstriction. Lipid breakdown, coronary and bronchial dilation. Breakdown of glycogen.

Question 18

Prazosin

Answer 18

Antagonist to alpha 1

Question 19

Yohimbine

Answer 19

Antagonist to alpha 2.

Question 20

Propranolol

Answer 20

Antagonist to beta1 and 2.

Question 21

Phorbol esters

Answer 21

Activate protein kinase C.

Question 22

Glucagon

Answer 22

Binds to glucagon receptor and leads to lipolysis, decreased glycogen synthesis, increased glycogen breakdown.

Question 23

How to treat early phase of asthma attack?

Answer 23

Beta 2 agonist, CysLT receptor antagonists, theophylline (adenosine antagonist and PDE inhibitor). Muscarinic antagonist.

Question 24

How to treat late phase asthma attack?

Answer 24

Glucocorticoids via a nuclear receptor to inhibit inflammation. Can inhibit wound healing, bone repair, and cause bone loss. CysLT receptor antagonists and long last beta 2 agonists. 5-lipoxygenase inhibitor reduces allergen-stimulated leukotriene production.

Question 25

Treatment for hypertension, angina and cardiac arrhythmias.

Answer 25

Beta receptor antagonists. Alpha 1 receptor antagonists. Calcium channel blockers.