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Ayahuasca: alkaloids, plants & analogs
assembled by Keeper of the Trout
Section 1 :
Pharmacology of Harmaline

Toxicity:
LD50:
120 mg/ kg/ sc/ rat Usdin & Efron 1979 cited Merck Index. Seventh
120 mg/ kg/ sc/ mouse Usdin & Efron 1979 cited Barnes & Eltherington 1965
In the rabbit, the "lethal dose" of harmaline was said to be 20 mg/kg iv by Fuentes & Longo 1971

Dosage:
100 mg or above as an oral activator for DMT or 5-MeO-DMT. Ott 1993
150-300 mg oral: Shulgin & Shulgin 1997

Duration:
3-4 [-?] hours. See comments under harmine above. It is likely that harmaline lasts slightly longer and takes longer to be excreted than harmine. It is processed and metabolized differently than harmine by the body due to enzyme specificity differences.

Pharmacological activity: (See also Harmine)
Hallucinogenic. Usdin & Efron 1979 citing Hochstein & Paradies 1957, who simply found it to be a component of a hallucinogenic brew. Hochstein and Paradies did not evaluate or determine its activity in any way.)
Also in Clarke's citing no reference for the claim
MAOI. Burger & Nara 1965
Harmaline given ip at 5 mg.kg causes 100% MAOI inhibition by 2 hours after injection and the activity drops rapidly after that. McKenna et al. 1998 cited Udenfriend et al. 1958
It is thought that half of this dose is effective for this purpose. McKenna et al. 1998
Vasodilator. Raymond-Hamet 1941
Therapeutic category: Amine oxidase inhibitor; Central stimulant. Merck Index
Gunn 1935 reported a clonic convulsant action followed by a depressant action
Psychoactive above 1 mg/kg iv or 4 mg/kg oral. Ott 1993 citing Naranjo 1967
This alkaloid MAY be hallucinogenic if extremely high doses are used. Physical distress is pronounced at these levels. Much of the resolution difficulties concerning the question of whether this alkaloid is hallucinogenic stem from semantic differences in defining ‘hallucinogenic'. There is wide variation between the lines that are drawn by different people, especially if comparing the ‘experienced' user with the ‘naive' professionals who often study them.
See also Ho 1977
20 mg/kg iv in monkeys caused pronounced tremors that occurred within a few minutes and lasted ~30 minutes. Tonic convulsions followed by clonic convulsions in rapid succession, nystagmus, inability to fix stare, excessive salivation & increased heart rate were reported. Head twitching began ~30 minutes after injection and continued for ~2 hours. Lethargy, weakness & incoordination were still visible at 2 hours and remained so until 4 hours after injection. Ho et al. 1970a
Shows antibacterial activity. Coulthard 1933
Harmaline was shown to have antibacterial activity but less so than harmine. (Ross et al. 1980 claimed harmaline was active but harmine was inactive.) Ahmad 1992

Pharmacokinetics:
Cmax (average) 6.3 ± 3.1 ng/ml
Tmax (average) 145.0 ± 66.9 min.
(Dosage of 0.4 mg/ kg oral as a component of hoasca) Callaway et al. 1999

Metabolism:
See Ho et al. 1971 & Ho 1977
Rats excrete as glucuronide conjugate. Ho et al. 1971

Distribution (in monkey brain):
High levels rapidly appeared in the cortex, hippocampus, caudate nucleus, putamen, cerebellum, fastigal nucleau, dentate nucleus, thalamic nuclei, pons & hypothalamus 15 minutes following intravenous injection of 20 mg/kg. The frontal white matter also showed substantial levels.
At 1 hr. there was almost even distribution in brain.
Reversal in distribution between white and grey matter was noted at 4 hours. (Level of unchanged harmaline was 73% versus 78% at 15 minutes)
Ho et al. 1970a

More animal studies:
Battista et al 1970
Fuentes & Longo 1971
Lamarre et al. 1971
Lamarre & Mercier 1971 & 1972
Llinás & Volkind 1972
Soirier et al. 1966
Udenfriend et al. 1958
Villablanca & Riobo 1970