Pharmacology of Drugs of Abuse (Amphetamine and Analogs)

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What is Amphetamine Psychosis?
This is when the individual, most likely the first time user, takes the drug and experiences confusion and disorientation.

What is Amphetamine psychosis?
This is when the individual takes the drug, usually several days in a row, and experiences schizophrenic symptoms such as hallucination, sterotyped behavior, aggression and etc. Increase in dosage is also done to achieve the same initial high.

Why does tolerance develops?
Tolerance develops because of the euphoric feeling that occurs after administration of the drug which is a positive reinforcement to continue taking. After continuous use, a higher and higher dose is required in order to produce the same pharmacological effects of the drug.

Why does dependence occur?
Dependence occurs as a form of avoidance from the psychological and physiological effects after the drug is removed. Depression and lethargy are some of the symptoms involved in withdrawal and users want to avoid these feelings.

What causes these effects of withdrawal?
Decrease of DA in the synaptic cleft during withdrawal.

What is the differentiating factor of amphetamine with other drugs?
Amphetamine is a neurotoxin and with chronic usage can cause permanent changes in dopaminergic neurons and the mesocorticolimbic DA pathway which exacerbates the withdrawal effects and makes it more difficult to maintain sobriety.

Talk about the pharmacokinetics of amphetamine.
Amphetamine can cross the blood brain barrier and effect the mesocorticolimbic DA system pretty favorably. In order for amphetamine to be removed from the system, individuals must urinate and by decreasing the pH of the urine, amphetamine can be removed at a quicker pace because it is a base.

What is the half life of amphetamine?
5 hours and can go upwards of 20-30 hours depending on the pH of the urine.

What is amphetamine deaminated into?
Oxidative deamination metabolizes amphetamine into p-hydroxyamphetamine.

In what forms does amphetamine exist in?
Amphetamine exists in D, L or racemic mixture. Its highly addicitve and a potent CNS stimulant.

Why is it widely used?
Because of the euphoria it provides at a low cost.

Why is methamphetamine more potent?
Because it has an extra methyl group making it more lipophilic which can easily cross the blood brain barrier.

What are the central effects of Methamphetamine?
Euphoria, locomotor stimulation, stereotyped behavior, anorexia.

What are the peripheral effects of Methamphetamine?
Vasoconstriction, High Blood pressure, GI motility decreased, bronchodilation.

What are the clinical uses for methampethamine?
Methamphetamine was first used as a bronchodilator to treat asthma and was also used to treat depression and schizophrenia. In addition, it was prescribed to treat heroine addiction as well as to alleviate parkinson’s disease.

Fact
The structure of a compound determines the pharmacological and therapeutic use as well as its side effects. It also determines the action of the amine.

What is different between meth and amphetamine in the way they interact with the cell?
Amphetamine and Meth utilize the DAT, SERT and NET but methamphetamine can also diffuse into the cell, releasing more dopamine.

Which is more potent, meth or ephedrine?
Meth

What are potential uses of methampethamine?
Pressor agent, CNS stimulant, A nasal decongestant. But are rarely used because of the potential harm.

What are the routes of administration?
Snorting, IV injection and Smoking

What is so dangerous about methamphetamine?
Its a cheap drug that provides an extreme euphoria, increases libido and energy. When smoked or injected it creates the most intense high and is taken in binge cycles. This means that once the high has been reached and euphoria has ended, it is smoked again. This occurs when methamphetamine is still in the body which increases its concentration and can become deadly.

Talk about the tolerance of methamphetamine.
Tolerance can build fairly quickly and the individual can go on a binge cycle with no sleep or food which is the most dangerous part of the drug use period. They increase dosage to obtain same high. Cocaine and meth effects are very similar.

Methamphetamine Japan experiment and why its ideal to experiment there.
Japan is ideal because they only used that one drug and did not mix it with others so obtained results solely on methamphetamine. Chronic use showed aggressive behavior, agitation, paranoia and hallucination. Short term use showed that its a CNS stimulant and increases activity.

What are some of the short term effects of methamphetamine?
Increased activity/alertness, euphoria and decreased fatigue.

What are the withdrawal symptoms of methamphetamine?
Severe cravings for drug, depression, anxiety and fatigue.

What is happening at the extracellular and intracellular matrices for methamphetamine use?
Although the extracellular matrix has low DA concentration, intracellularly there is the same amount but there is inhibition via auto-receptors of the DA neuron to fire because of the increased release in DA that occurred. DA neurons decrease in the brain as well as 5HT.

Talk about the half life of methamphetamine.
The half life can vary depending on the rate of administration. Methamphetamine is first metabolized to amphetamine and then undergoes oxidative deamination to p-hydroxyampethamine which is why the half long is longer than that of amphetamines.

Talk about the mechanism of amphetamine.
Amphetamine, methamphetamine and MDMA are all substrates to the 5HT, NE and DA transporters and enhance neurotransmitter release. Methamphetamine and MDMA can both diffuse into the cell. MDMA however has the greatest affinity to the 5HT receptor. The combination of 5HT and DA release causes hallucinations.

What are the central effects of MDMA?
Locomotor activity increase, dose dependent body temperature increase, increased motivation and alertness.

What is the most fatal effect of MDMA?
Hyperthermia. Occasional users can experience minor impairments while the chronic user can experience kidney failure, immune system compromised, sexual dysfunctions and cognitive impairments.

Neurotoxicity of MDMA.
PET scans show that there are permanent impairments in the 5HT 2A receptor which will not be corrected with abstinence. Causes long lasting effects on the markers.

Why is it difficult to study MDMA causes in humans?
Because most humans take MDMA with other drugs, such as marijuana and alcohol and the effects of MDMA alone are hard to determine.

What are the long term and short term effects?
Short term is that there is a massive increase in 5HT and long term is that there is marked decrease in 5HT release.

What are the four effects that contribute to neurotoxicity?
Hyperthermia, Metabolism of MDMA, Oxidative stress and Metabolism dysregulation caused by mitochondrial dysfunction.

What are the structures rich in serotonin?
There are many subtypes and they all produce different responses. GI tract, Blood vessels, platelets, Nerve Endings.

What are the four effects of MDMA on the serotonin system?
1) MDMA is transported into the cell through the 5HT carrier. 2. MDMA inhibits reuptake of 5HT. 3. MDMA increases serotonin release. 4. MDMA inhibits tryptophan hydroxylase.

What are the effects of temperature on tryptophan hydroxylase?
When treating with MDMA at room temperature there is a hyperthermic response and tryptophan hydroxylase decreases. Treating at 6 degrees theres a hypothermic response and no reduction in tryptophan hydroxylase.

Does MDMA inhibit MAO.
Yes

What is the peak release of DA after MDMA and return to baseline?
Peak release is 120 min after and returns to baseline at 180 min.Free radical formation increases in the brain.

MDMA and the serotonin syndrome. What are the behavioral response caused by release of 5HT and DA?
1. Hyperactivity 2. Ejaculation 3. Salivation 4. Head bobbing 5. Penile erection

What does acute injection of MDMA do?
Acute injection causes cerebral concentration of 5HT to decline due to neurotoxic damage to the 5HT nerve ending. There is slight recovery of 5HT after injection in the first few hours though.

What are the hallucinogenic effects of MDMA?
Reduces negative thoughts, increases empathy, euphoria, openness and relaxation. Sounds and colors are more intense and is classified as a psychedelic drug. Most psychedelics are related to the 5HT.

What are the responses to the psychedelic drugs?
Heightened awareness, a feeling that self is divided, environment is beautiful, attention turned inward and that everything takes on great meaning and truth. There is also diminished ability to determine boundaries between people and objects.

What are the three criteria to categorize LSD type drugs?
Subjective effects, cross tolerance between compounds and response to selective antagonists. However, because there is no cross tolerance between LSD and amphetamines, MDMA is classified in its own group.

Reinstatement of MDMA.
The euphoria and self confident is remembered. MDMA has weaker reinforcer than meth but nonetheless it does its job.

Pharmacokinetics of MDMA.
Well absorbed orally. Novices take 1-2 pills, experienced take 3+. Difference implies tolerance. Onset of action is 20 min. Peak affect is 60-90 min and duration of action is 5 hours.

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