Ergot alkaloids effects

Hindmarch I, Parrott AC and Lanza M (1979). The effects of ergot alkaloid derivative (Hydergine) on aspects of psychomotor performance, arousal, and cognitive processing ability. Journal of Clinical Pharmacology, 19, 726-732. 

In his general studies aimed at the synthesis of ergot alkaloids, Hegedus effected the coupling of dihaloindole 79 with the zinc reagent 80, generated in situ from l-methoxy-l,2-propadiene, to afford ketene 81 [21],... 

Ergotamine is an ergot alkaloid indicated in the treatment of migraine. Ergotamine has marked vasoconstrictor effects. 

Coadministration of ritonavir with certain nonsedating antihistamines, sedative hypnotics, antiarrhythmics, or ergot alkaloid preparations may result in potentially serious and/or life-threatening adverse reactions due to possible effects of ritonavir on the hepatic metabolism of certain drugs (see Contraindications). 

Dopamine (Intropin) [Vasopressor/Adrenergic] Uses Short-tOTn use in cardiac decompensation secondary to X contractility when no hypovolemia is present T organ p fusion (at low dose) Action Renal dose 2-5 mcg/kg/min Inotropic dose 5-10 mcg/kg/min Pressor dose >10 mcg/kg/min Dose Adults Feds. 5-20 mcg/kg/min by cont inf, start at 5 and t by 5 mcg/kg/min to 20 mcg/kg/min max to effect (mix 400 mg in 250 mL DjW to make 1600 mcg/mL) (see Table 1-3) Caution [C, ] Contra Pheochromocytoma (adrenal gland tumor), VF, sulfite sensitivity Disp Inj 40, 80, 160 mg/mL, premixed 0.8, 1.6, 3.2 mg/mL SE Tach, vasoconstriction, 4- BP, HA, N/V, dyspnea Notes >10 mcg/kg/min X renal p fiision Interactions t Effects W/ a-blockers, diuretics, ergot alkaloids, MAOIs, BBs, anesthetics, phenytoin X effects W/ guanethidine EMS Correct hypovolemia before use use microdrip set or inf pump check soln- discolored... 

Uses Postpartum bleeding (uterine subinvolution) Action Ergotamine derivative Dose 0.2 mg IM after placental deliv y, may repeat 2-4-h intervals or 0.2-0.4 mg PO q6-12h for 2-7 d Caution [C, ] Contra HTN, PRO Disp Inj, tabs SE HTN, N/V Interactions t Vasoconstriction W/ ergot alkaloids, sympathomimetics, tobacco EMS Tobacco use can t vasoconstriction and lead to a hypertensive crisis OD May cause N/V/D, chest/abd pain, limb numbness, and possibly distal gangrene d/t vasoconstriction activated charcoal may be effective for PO form... 

Mechanism of Action An ergot alkaloid that centrally acts and decreases vascular tone, slows heart rate. Peripheral action blocks alpha-adrenergic receptors. Therapeutic Effect Improved Oj uptake and improves cerebral metabolism. Pharmacohinetics Rapidly, incompletely absorbed from GI tract. Metabolized in liver. Eliminated primarily in feces. Half-life 2-5 hr. 

A wide variety of drugs with actions at other receptors (eg, a adrenoceptors, Hi-histamine receptors) also have serotonin receptor-blocking effects. Phenoxybenzamine (see Chapter 10) has a long-lasting blocking action at 5-HT2 receptors. In addition, the ergot alkaloids... 

In addition to the effects noted above, the ergot alkaloids produce a variety of other central nervous system and peripheral effects. Detailed structure-activity analysis and appropriate semisynthetic modifications have yielded a large number of agents of interest. 

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