Pharmacology Test 2: Marijuana And Hallucinogens

Front 1

Marijuana is derived from?

Back 1

Cannabis sativa

Front 2

principal psychoactive component of marijuana

Back 2

1-delta9-tetrahyrocannabinol (THC)--- Dronabinol is available as an oral prep.

Front 3

synth. analog of THC with anti-emetic properties?

Back 3

Nabilone.

Also nantradol (not FDA approved)

Front 4

~ THC content of one marijuana cigarette?

Back 4

about 10-50 mg, with dose ranging from 5-25 mg.

Front 5

Peak plasma level time?

Back 5

10-30 min after smoking

Front 6

Decay properties of marijuana?

Back 6

two componenet cure. Initial redistribution to adipose (45 minutes), and then gradual metabolism of THC and elimination (t1/2 4 days).

Front 7

Metabolism of THC

Back 7

most in the liver, and many oxygenative metabolic products continue to have psychoactive effects.

Front 8

Active Metabolites of THC?

Back 8

11-hydroxy-THC, potency comparable to THC. Other less potent metabolits as well.

Front 9

importance of oxygenated metabolites?

Back 9

oral intake of THC and 'first pass' results in high 11-OH THC metabolites, while THC itself is in low concentration.

Front 10

Excretion of THC

Back 10

90% THC excreted in urin and feces within 5 days. Remaining metabolites take longer due to renal reabsorption, FA trapping, tissue distribution etc.

Front 11

What does urinalysis look for?

Back 11

THC and 9-carboxy metabolites.//

If recent use, then THC higher than 9-COOH. Slow excretion of 9-COOH allow detection of THC use for period of days to weeks.

Front 12

Effects of single dose THC?

Back 12

tachycardia (no change in BP though), euphoria (perceptual distortions, altered perceptions, NO hallucinations at this dose).

relaxation and sedation (unlike with LSD).//

psychomotor impairment: imparied STM, complex motor affected ie. driving, flying.

dry mouth, hunger, peripheral vasodilation (pink conjunctiva), bronchodilation.

Front 13

effects of higher dose of THC?

Back 13

confusion, disorganized thinking, hallucinations, delusions; euphoria turns to anxiety, panic and paranoia. More like to occur with ORAL admin. b/c of lack of control.

Front 14

THC Mech of action?

Back 14

CB1 and CB2 receptors. CB1 mainly in CNS, and CB2 periphery. They are similar to G protein coupled receptors.

Front 15

Mech of action through CB receptors?

Back 15

inhibit AC. CB1 present in high concentration in hippocampus and cortex, striatum and Nuc. Acc. Thus influencing memory, congnition, motor fxn, and reinforcement.

Front 16

What are the endogenous ligands for CB-Rs?

Back 16

Anandamide (arachidonly-ethanolamide), arachidonyl-glycerol.

Front 17

Anandamide and arachidonyl glycerol ligands location and purpose???

Back 17

anadamide, a lipid identified in brain and some peripheral tissues.//

arachidonyl-glyercol found in hippocampus.//

thought to function in extinction of learned fearful memories.//

Front 18

Therapeutic use of THC?

Back 18

reduction of intraocular pressure in glaucoma, chemotherapeutic drug induced vomiting (FDA approved; dronabinol and marijuana), pain relief?,

Front 19

What's CB1 antagonist that reduces replase in chronic tobacco smokers and gives weight loss in obese subjects?

Back 19

Rimonabant (not FDA approved yet)

Front 20

Tolerance and dependance on marijuana?

Back 20

slow dev'p of tolerance, weak cross-tolerance to Ethanol, not to LSD-like drugs. Little evidence of dependance.// Craving for THC after withdrawal from heavy use.//

Front 21

Sxs from chronic marijuana use?

Back 21

bronchitis, asthma, , possible role in lung cancer development, immune suppression, decreased gonadotropins and sex steroids, amotivational syndrome, severe memory loss.//

Front 22

Lysergic acid diethylamide (LSD)

Back 22

hallucinogen, synthetic drug. No therapeutic use. very potent, action duration upto 12 hours.

Front 23

Effects of LSD?

Back 23

somatic (1-2 hrs) dizziness, pupil dilation, weakness, tremor.//

perceptual (2-6 hrs): blurred vision, diff. focusing, altered awareness of colors, shapes, hallucinations.//

affective sxs: euphoria OR dysphoria, depression, fear paranoia. Panic (2-5 hrs) after 6 hrs, detachment.

Front 24

LSD mode of action?

Back 24

incompletely understood: partial agonist at 5HT2-R.

Front 25

How are LSD effects reversed?

Back 25

use 5HT2-R antagonists, and partially by AD D2-R antagonists.

Front 26

What's Psilocybin

Back 26

LSD related, from mushrooms.

Front 27

Amphetamine analogues aka 'designer drugs'.

Back 27

MDMA aka 'ecstasy'. Known as rave drug, general mood elevation.

Mescaline, related drug found in peyote cactus.

Front 28

What happens with increaing bulk of substituents on aromatic ring of amphetamine?

Back 28

causes a transition from amphetamine-like stimulation to LSD like hallucinogentic action.

Front 29

Anticholinergic hallucinogens?

Back 29

atropine, scopolamine. Especially in elderly pts.

**phenothiazines, with atropine-like side effects, contraindicated in treatment of anticholinergic delirium.

Front 30

Phencyclidine (PCP)

Back 30

synthetic drug, intended to be an anesthetic. 40% pts develop dysphoric rxn and some overt psychotic state. //

Ketamine is a related drug.

Front 31

PCP Mech of action

Back 31

PCP and ketamine are non-competitive channel blockers at NMDA-R, blocking influx of Ca.

Front 32

Acute actions of PCP

Back 32

taken orally or by smoking: intoxication in 2-5 min, blank stare, muscular rigidity, hypersalivation, sweating last upto 24 hrs. High doses: unpredictable, bizzare aggressive behaviour, comatose state for 4-6 hrs.

Front 33

PCP Chronic uSe

Back 33

difficulty thinking, memory deficit, speech impairment, intensify psychotic behavior in schizophrenics.

Front 34

PCP Tx of OD.

Back 34

symptomatic, talk-down not effective, Tx convulsions with diazepam, hypertension with hydralazine, and psychotic episodes with haloperidol. * avoid anticholinergic phenothiazines.//