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Methaqualone

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4 sources

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Collated from PsychonautWiki, TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.

Sections
DepressantQuinazolinoneHabit-formingPW

Also known as Methaqualone, Quaaludes, Ludes, Mandrax, Sopor, Quack, Vitamin Q, Soaper, qualudesPW

Fatal overdose may occur when GABAergic substances are combined with other depressants such as opiates, benzodiazepines, barbiturates, gabapentinoids, thienodiazepines or alcohol.[1] It is strongly discouraged to combine these substances, particularly in common to heavy doses.PW

Addiction potentialPW
extremely addictive
ToxicityPW
doses of over 300mg can be dangerous for first time users; safe at appropriate dosages
TolerancePW
full tolerance within a couple of days of repeated administration; half after 3 - 7 days; baseline after 1 - 2 weeks
Cross-tolerancePW
GABA|gabaergic, depressants

Oral

Route dataPsychonautWiki

Dose
WeakerStronger
ThresholdLightCommonStrongHeavy
75 mg150–300 mg300–500 mg500–600 mg—+
0600 mg
LightCommonStrongHeavy
Duration
ShorterLonger
Peak2–4 hours
Offset2–4 hours
Total5–8 hours
After-effects6–8 hours
OnsetCome-upPeakOffset

Smoked

Route dataPsychonautWiki

Dose
WeakerStronger
ThresholdLightCommonStrongHeavy
50 mg50–100 mg100–200 mg200–300 mg—+
0300 mg
LightCommonStrongHeavy
Duration
ShorterLonger
Total1–2 hours

Dangerous interactionsPW

DepressantsDissociatives

Caution / uncertainPW

Stimulants

🧬 Receptor activityDC

TargetActionAffinitySource
GABA A receptor alpha-2/beta-2/gamma-2 (GABRG2)Positive allosteric modulator4.61 EC50DRUGCENTRAL
GABA A receptor alpha-3/beta-2/gamma-2 (GABRG2)Positive allosteric modulator4.31 EC50DRUGCENTRAL
GABA A receptor alpha-4/beta-2/delta (GABRD)Positive allosteric modulator4.17 EC50DRUGCENTRAL
GABA A receptor alpha-4/beta-3/delta (GABRA4)Agonist3.91 EC50DRUGCENTRAL
GABA A receptor alpha-5/beta-2/gamma-2 (GABRG2)Positive allosteric modulator4.56 EC50DRUGCENTRAL
GABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1)Positive allosteric modulator4.41 EC50DRUGCENTRAL
GABA-A receptor alpha-1/beta-3/gamma-2 (GABRA1)Positive allosteric modulator4.52 EC50DRUGCENTRAL
GABA-A receptor alpha-6/beta-2 (GABRA6)Positive allosteric modulator4.13 EC50DRUGCENTRAL
GABA-A receptor alpha-6/beta-2/delta (GABRB2)Positive allosteric modulator4.44 EC50DRUGCENTRAL
GABA-A receptor alpha-6/beta-3/delta (GABRD)Positive allosteric modulator4.5 EC50DRUGCENTRAL
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Mechanism of actionPH

IN ADDITION TO SEDATIVE-HYPNOTIC PROPERTIES ... /IT/ POSSESSES ANTICONVULSANT, ANTISPASMODIC, LOCAL ANESTHETIC, & WEAK ANTIHISTAMINIC PROPERTIES. IN HIGH DOSES IT SELECTIVELY DEPRESSES POLYSYNAPTIC PATHWAYS IN THE SPINAL CORD. THE DRUG HAS ANTITUSSIVE ACTIVITY COMPARABLE TO THAT OF CODEINE ... IT LACKS ANALGESIC ACTIVITY.

Pharmacokinetics

Half-lifePH

2-3 hr /From table/

AbsorptionPH

IN MAN, 99% OF METHAQUALONE IS ABSORBED IN 2 HOURS. IN THE PLASMA, 70 TO 90% IS BOUND TO ALBUMIN. ... METABOLITES ... ARE MAINLY CONJUGATED AND EXCRETED IN THE URINE, BUT THE 4-HYDROXY METABOLITE IS EXCRETED INTO BILE. THE PHARMACOKINETICS IS THAT OF A TWO-COMPARTMENT SYSTEM, WITH A DISTRIBUTION HALF-LIFE OF LESS THAN 1 HOUR AND AN ELIMINATION HALF-LIFE OF 10 TO 40 HOURS.
AFTER ABSORPTION METHAQUALONE IS TAKEN UP BY ADIPOSE TISSUE & GRADUALLY RELEASED OVER PERIOD OF SEVERAL DAYS. AS IT IS RELEASED IT RAPIDLY UNDERGOES GLUCURONIDE CONJUGATION ... & IS EXCRETED EQUALLY IN URINE & FECES FOR UP TO 6-7 DAYS. IN TOXIC DOSES UNMETABOLIZED METHAQUALONE IS ALSO FOUND IN URINE.
BLOOD & URINE SAMPLES FROM ACUTELY INTOXICATED PATIENT STUDIED. 4 MAJOR MONOHYDROXYLATED METABOLITES FOUND CONJUGATED IN URINE. 2-METHYL-3-[2-(HYDROXYMETHYL)PHENYL]-4(3H)-QUINAZOLINONE FOUND UNCONJUGATED IN URINE & BLOOD.
URINARY EXCRETION OF 5 C-MONOHYDROXY METABOLITES & METHAQUALONE N-OXIDE MEASURED FOLLOWING ORAL ADMIN OF 250 MG TO GERIATRIC PT. TOTAL EXCRETION OF 6 METABOLITES IN 24 HR WAS APPROX ONE-HALF THAT IN GROUP OF YOUNG, HEALTHY ADULTS.
For more Absorption, Distribution and Excretion (Complete) data for METHAQUALONE (10 total), please visit the HSDB record page.

MetabolismPH

MORE THAN 99% OF THE DRUG IS METABOLIZED BY THE HEPATIC MICROSOMAL SYSTEM, AND 4-HYDROXYMETHAQUALONE AND THE N'-OXIDE ARE THE MAJOR PRIMARY METABOLITES. AT LEAST EIGHT OTHER HYDROXYL METABOLITES ARE FORMED.
YIELDS 3-(3-HYDROXY-2-METHYLPHENYL)-2-METHYL-4(3H)-QUINAZOLINONE, 3-(4-HYDROXY-2-METHYLPHENYL)-2-METHYL-4(3H)-QUINAZOLINONE, & 6-HYDROXY-2-METHYL-3-(O-TOLYL)-4(3H)-QUINAZOLINONE IN MAN. /FROM TABLE/
... METHAQUALONE ... GAVE 2-NITROBENZO-ORTHO-TOLUIDIDE ... AS HUMAN URINARY METABOLITE.
BIOTRANSFORMATION ... WOULD BE EXPECTED TO PROCEED BY HYDROXYLATION, & THIS LARGELY OCCURS IN PRACTICE, WHEN GLUCURONIDES OF ... 2-METHYL-3-(3-HYDROXY-2-METHYLPHENYL)-4(3H)-QUINAZOLINONE, 2-METHYL-3-O-TOLYL-6-HYDROXY-4(3H)-QUINAZOLINONE & 2-METHYL-3-O-TOLYL-8-HYDROXY-4(3H)-QUINAZOLINONE ... EXCRETED IN URINE OF ... RATS.
For more Metabolism/Metabolites (Complete) data for METHAQUALONE (7 total), please visit the HSDB record page.
Methaqualone has known human metabolites that include hydroxy-methaqualone.

Plan when to take Methaqualone — see where onset, peak and comedown land on the clock

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.