Human Aspects of Cardiovascular And Renal Pharmacology

Question 1

Amyl Nitrite

Answer 1

Potent vasodilator, lower blood pressure due to being converted to NO. Used to treat agina.

Question 2

Bisoprolol

Answer 2

It is a selective B1 adrengergic receptor blocker. Used to limit the dmaging effects of chronic catecholamine stimulation (toxicm causes cell death) and to imrpove cardiac function.

Question 3

Clofibrate

Answer 3

Fibric acid derivative, lowers VLDL and LDL to a lesser extent. Stimulates lipoprotein lipase , releasing triglycerides from VLDL and chylomicrons -> lipids taken up and stored in fat or metabolised.

Question 4

Colestyramine

Answer 4

Anion exchnage resin - prevents reuptake of bile acid from the intestine causing an increase in cholesterol metabolism to synthesise bile aicd in the liver. Cholesterol taken up from blood to maintain enterohepatic pool.

Question 5

Doxazosin

Answer 5

Commonly used alpha antagonist. Dilates resistance and capacitance vessels. Lack of block of alpha2, only apha 1 so no marker tachycardia.

Question 6

Ezetimibe

Answer 6

Inhibits intestinal absorption of cholesterol - binds to blocks a sterol transporter on the brush border membrane of the intestinal epithelial cells (NPC1L1). Circulates enterohepatically so repeated re-delivered to intestine.

Question 7

Flecainide

Answer 7

Class 1C antidysrhythmic - very slow to associate and dissociate from the VGNa+ channels. Good at supressing ectopic beats but also nearly suppress everything else as well - pro-dysrhythmic. Higher mortality rate than placebo. Only used in unusual circumstances.

Question 8

Glyceryl Trinitrate

Answer 8

Organic nitro derivatives - used to treat angina in acute attakcs. Taken sublingually. Cause vasodilatation as converted to NO in vascular smooth muscle cells. Cause venous dilatation and operate on collaterol blood vessels (as arterioles already fully dlated).

Question 9

Hydralazine

Answer 9

Direct acting smooth muscle relaant used to treat hypertension - vasodilator in arterioles and arteries. Decrease afterload. Antihypertensive used in combination with a beta-blocker.diuretic.

Question 10

Hypoxia-inducible Factor-1a (HIF-1a)

Answer 10

Regulate expression of multiple angiogenic genes (including VEGF). New blood flow to myocardial ischaemic tissue.

Question 11

Isosorbide Dinitrate

Answer 11

Nitrovasodilators - converted to NO and acts on venules and collateral blood vessels in the heart. Treat angina.

Question 12

Ivabradine

Answer 12

Acts on the If current in the sinoatrial ode. Blocking this current reduces cardiac pacemaker activity, slowing the heart rate and allows more time for blood to flow to the myocardium. Few side effects. Treats angina.

Question 13

Labetalol

Answer 13

It is an alpha1, Beta1 and beta2 antagonist but more beta than alpha. Antihypertensive.

Question 14

Moxonidine

Answer 14

Centrally acting antihypertensive drug. Selective agonist at the imidazoline receptor subtype 1 -> decrease in sympathetic activity and a decrease in blood pressure. Greater affinity for I1 receptor than the a2 receptor. May also promote Na+ excretion.

Question 15

Nicotinic Acid

Answer 15

Inhibits liver triglyceride production and VLDL secretion. Increases levels of t-PA.

Question 16

Paclitaxel (Taxol)

Answer 16

In drug-eluting stents - antiproliferative drug. Interfers with the normal function of microtubule growth (otherwise get scar tissue developemtn into the lumen) so lumen stays clearer. Reduce restenosis (re-narrowing of the lumen)

Question 17

Phentolamine

Answer 17

Non-selective alpha blockade - gives vasodilatation and a marked reflex tachycardia. Antihypertensive agent. Blockade of CNS a1 receptors modulates barorecetpor reflex mechanism -> decreasing symapthetic discharge.

Question 18

Pindolol

Answer 18

Non-selective beta blocker with partial B adrenoceptor agonist activity. AT high doses it has similar effects to adrenaline (increase HR, BP). Antiarrhythmic effects as well.

Question 19

Rosiglitazone

Answer 19

PPARgamma agonist, reduces atherosclerosis. Induces LXR transcription, leading to indirect induction of ADBA1 expression. ABCA1 transfers cholesterol from non-hepatic peripheral tissues to HDH so that it can be transported to the liver to be destroyed.

Question 20

Simvastatin

Answer 20

Statin - inhibits HMG-CoA reductase - rat elimiting enzyme for cholesterol synthese -> liver takes up more LDL from blood , reduction in blood levels and less predisposition to atheroma formation.

Question 21

Sirolimus

Answer 21

Antiproliferative drug-eluting stent drug. Prevents restenosis.

Question 22

Sodium Nitroprusside

Answer 22

NO-releasing drug - used as a vasodilator to reduce blood pressure. Hypertension treatment.

Question 23

Trimetaphan

Answer 23

Antagonist at cholinergic nicotinic receptos blocking sympathetic nervous system activity - causes vasodilatation and lowers blood pressure. Reflex tachycardia.

Question 24

Vascular Endothelial Growth Factor (VEGF)

Answer 24

Causes development of new blood vessels at the site of expression - limited duration of transgene ezpression required as long term gives abnormal angiogenesis. New blood flow to ischaemic tissues. Myocardial infarction treatment.