Autacoids - Ergot

Question 1

What can act as an agonist, partial agonist, and antagonist at alpha adrenoceptors and serotonin receptors

Answer 1

Ergot alkaloids

Question 2

(Oral/IM) ___ dose of ergotamine is about 10 times larger than the (Oral/IM) ____ dose.

Answer 2

Oral, IM (but speed of absorption and peak blood levels after oral administration can be improved by CAFFEINE)

Question 3

Preparations of ergotamine include (rectal, buccal, aerosol, AOTA)

Answer 3

AOTA

Question 4

Which ergot alkaloid subgroup produces marked and prolonged _-receptor-mediated vasoconstriction

Answer 4

Vasoselective (ergotamine is the prototype)

Question 5

Which ergot alkaloid subgroup produces powerful contraction in this tissue, especially near term?

Answer 5

Uteroselective (ergonovine is the prototype)

Question 6

Which semisynthetic prototypical hallucinogenic ergot derivative (subgroup) is a potent 5-HT2 blocker in peripheral tissues, its actions in the CNS are thought to be due to agonist actions at dopamine receptors?

Answer 6

CNS selective (bromocriptine, pergolide are the prototype)

Question 7

Which ergot alkaloid is the main treatment of acute attacks of migraine and improved when taken with caffeine?

Answer 7

Ergotamine (BUT Triptan is first line for migraine because of lower toxicities)

Question 8

Which ergot alkaloid reduces prolactin secretion and pituitary tumor?

Answer 8

Bromocriptine, pergolide, cabergoline

Question 9

Which ergot alkaloid reduces postpartum bleeding?

Answer 9

Ergonovine and ergotamine (BUT don’t give before delivery of placenta)

Question 10

Which ergot alkaloid is used for the treatment of Parkinson’s disease?

Answer 10

Bromocriptine and cabergoline

Question 11

Which ergot alkaloid is used to produce prompt vasoconstriction during coronary angiography to diagnose variant angina and given via IV?

Answer 11

Ergonovine

Question 12

Which ergot alkaloid is used to relieve senility and treat alzheimer’s disease?

Answer 12

Dihydroergotoxine

Question 13

Give the side effects of ergot alkaloid on vascular, gastrointestinal, uterine and CNS systems?

Answer 13

Vascular: prolonged vasocon - ischemia, necrosis; GI upset; Uterine contractions; CNS hallucinations (psychosis like)

Question 14

Autacoids with significant actions on vascular smooth muscle as well as other tissues.

Answer 14

Vasoactive Peptides

Question 15

Give 5 drugs that are RAAS antagonists which are for hypertension?

Answer 15

Aliskiren, Captopril, Enalapril, Losartan, Valsartan, other ARBs?

Question 16

Decreases renin, angiotensin I, II, aldosterone | Toxicity: angioedema, renal impairment

Answer 16

Aliskiren

Question 17

Inhibits ACE, decreases angiotensin II, aldosterone | Increases Bradykinin | Toxicity: Cough, terarogenic, hyperkalemia

Answer 17

Captopril, Enalapril

Question 18

AT1 inhibitor, decerases angiotensin II | Toxicity: teratogenic, hyperkalemia

Answer 18

Losartan, Valsartan, other ARBs

Question 19

Kinin Antagonist that inhibits kallikrein, bradykinin || Treats: Hereditary angioedema || Toxicity: Hypersensitivity

Answer 19

Ecallantide

Question 20

Kinin Antagonist that blocks B2 bradykinin receptor || Treat: hereditary angioedema | Toxicity: Hepatotoxic, hypersensitive

Answer 20

Icatibant

Question 21

Endothelin antagonist on ETa, ETb receptors | Treat: Pulmonary hypertension | Toxicity: Hepatic, possible teratogen

Answer 21

Bosentan, Macitentan

Question 22

Neurokinin antagonist on Tachykinin NK1 receptor | Treat: (antiemetic) for chemo-induced vomiting | Toxicity: Asthenia, hiccup

Answer 22

Aprepitant

Question 23

Neurokinin antagonist which releases substance P from nerve endings || Treat: joint pain, neuralgia (topical) || Toxicity: Burning, stinging, eryhtema

Answer 23

Capsaicin

Question 24

Block renin secretion (alpha agonists)

Answer 24

Clonidine,Methyldopa

Question 25

Angiotensin converting enzyme inhibitors

Answer 25

Captopril(prototype),Enalapril