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20 Cards in this Set

  • Front
  • Back

Why are drugs that increase regional blood flow used and in which diseases are they relevant?

To enhance perfusion to organs that require more perfusion or has been compmrimised due to vasospasm or atherosclerosis.




Peripheral artery disease, Raynaud phenomenon, erectile dysfunction

What is the steal syndrome?

In cases where one artery is blocked by atherosclerosis, the drugs enhancing blood flow can make blood be routed to other arteries. Blood will be "stolen" from the ischemic region.

Which drugs can be used to treat Raynaud phenomenon?

Dihydropyridines:


nifedipine, nimodipine


Calcium blockers + antihistamines:


cinnarizine, flunarizine,


Adrenergic alpha agonists:


Phentolamine, prazosin

Which drugs can be used to treat peripheral artery disease?

Prostanoid analogues:


Alprostadil, iloprost


PDE inhibitors:


Cilostazol

Which drugs can be used to treat erectile dysfunction?

Sildenafil, alprostadil

Which calcium channel blockers are used to treat vasospastic diseases?

Dihydropyridines like nifedipine and nimodipine.

What is the mechanism of action of sildenafil?

Sildenafil inhibits phosphodiesterase type 5 (PDE5). This isoform of PDE is found in the corpus cavernosum (and the pulmonary circulation).When sexual stimulation the brain signals the corpus cavernosum to release NO. This activates guanylate cyclase, which forms cGMP which causes muscle relaxation in the corpus cavernosum, allowing blood to enter. These drugs inhibit PDE5 and therefore inhibit the degradation of cGMP, causing a stronger and longer-lasting erection.

What is the mechanism of action of cilostazol?

Cilostazol inhibit phosphodiesterase in RBCs, causing an increase in cAMP levels. This increases the deformity of the RBC membrane.

What are the side effects of sildenafil?

Hypotension with reflex tachycardia, headache, dizziness, flush. Sildenafil causes visual disturbances.

What is the mechanism of action of alprostadil?

Alprostadil is a synthetic prostaglandin E1 (PGE1). It increases the deformability of RBCs, inhibit platelet aggregation and enhances fibrinolysis. These changes enhance the microcirculation.

What is the mechanism of action of iloprost?

It is a synthetic prostacyclin I2 (PGI2). It induces vasodilation and inhibits platelet aggregation.

What is the mechanism of action of cinnarizine and flunarizine

These drugs are both calcium channel blockers and antihistamines.

What is the mechanism of action of prazosin and phentolamine?

These drugs block the alpha receptor-mediated vasoconstriction.

Name the drugs which can be used to treat obesity.

Orlistat, liraglutide, bupropion-naltrexone

What is the mechanism of action of orlistat?

Orlistat is a pancreatic lipase inhibitor. By inhibiting this enzyme, the absorption of ingested fat can be decreased. Up to 1/3 of ingested fats can be blocked from absorption.

What are the side effects of orlistat?

Steatorrhoea. Fat soluble vitamin deficiency. These side-effects can be reduced by reducing fat intake.

What is the mechanism of action of liraglutide?

Liraglutide is a GLP-1 derivative. It stimulates insulin release, inhibits glucagon release and slows gastric emptying. It’s primarily used in diabetics, but it is also effective in obesity if given in higher doses as it decreases hunger.

What is the mechanism of action of bupropion-naltrexone?

Bupropion is an antidepressant and smoking cessation drug. Naltrexone is an opioid receptor antagonist used to treat opioid dependence. Combined they have an appetite-suppressing effect.

Other treatments of obesity?

Decresing size of lumen of stomach with intra-gastric balloon or bariatric surgery.

When are drugs for treatment of obesity contraindicated?

In pregnancy or during lactation, unstable heart disease, severe hypertension and psychiatric disorders.