stimulants

Question 1

What are some stimulant drugs?

Answer 1

1. Amphetamines (benzedrine)
2. Cocaine
3. Ritaline (Methylphenidate)
4. MDMA (Ecstasy, molly)
5. Bath Salts (methlenedioxypyrovalerone, Mephedrone)
6. Xanthines like caffeine and theophylline

Question 2

What is a sympathomimetic?

Answer 2

A drug that acts as an agonist of the sympathetic NS

Question 3

What are some examples of amphetamines?

Answer 3

Adderall
speed
crystal meth

Question 4

What are some effects of amphetamines?

Answer 4

Excitement 
Euphoria 
Increase motor activity
Some increased cognitive function
Insomnia 
anorexia 
and adverse actions are anxiety, irritability and restlessness

Question 5

What is the mechanism of action of Amphetamines?

Answer 5

Reverses norepi and DA reuptake transporters to essentially push out more of these neurotransmitters into the synapse.

• also just blocks the reuptake transporter as well
• at high doses it blocks MAO (monoamine oxidase)
• It also interacts with VMAT-2

Question 6

What is VMAT-2?

Answer 6

It is a vesicle monoamine pump which is found on growing vesicles found in the presynaptic terminal.

• basically loads the vesicles full of neurotransmitters
• reversed by amphetamines

Question 7

What is the clinical use of amphetamines?

Answer 7

Treatment of ADHD
Narcolepsy
Past: weight loss and fatigue but not recommended

Question 8

What are some chronic adverse effects of amphetamines?

Answer 8

Amphetamine psychosis- which resembles schizophrenic attack with hallucinations, paranoia and aggressive behavior.

Question 9

Is there dependence on amphetamines?

Answer 9

Yes,
Strong psychological dependence: Insistent memory of euphoria
However, no clear cut withdrawal syndrome

Question 10

What is the mechanism of action of Ritalin?

Answer 10

Profound elevation of NE and DA

• Via inhibits NET and DAT transporters
• but does not enter cell to facilitate release of NT inside cell

Question 11

Other facts about Ritalin?

Answer 11

Only 20% enters the systemic circulation
peak level at about 2 hours
no euphoric response to drug- clinically very useful then
half life of 2-4 hours

Question 12

What is Ritalin used to treat?

Answer 12

ADHD

Question 13

What is the mechanism of action of Modafinil?

Answer 13

Increases DA Levels in striatum and nucleus accumbens through inhibition of DAT’s

• also increased 5-HT, Glutamate and histamine
• inhibits GABA release

Question 14

What does Modafinil used to treat?

Answer 14

Sleep apnea
Narcolepsy
shift work disorders
ADHD in adults

Question 15

What is the mechanism of action of MDMA?

Answer 15

Inhibits monoamine transporters, prinicpially 5-HT transporters. SERT’s

• also released Serotonin
• SSRI
• inhibits DAT’s and NET’s

Question 16

Is MDMA addictive and what can it be used for?

Answer 16

No

Treatment of PTSD and depression

Question 17

Sudden death or illness can happen when taking MDMA, this is due to what?

Answer 17

acute hyperthermia
excessive water consumption- which causes hyponatremia
- because 5HT is important in thermoregulation

Question 18

What is the mechanism of action of Cocaine?

Answer 18

Binds too and inhibits NET, DAT and SERT’s

• psychomotor stimulant
• also used as a local anesthetic

Question 19

What are some of the effects of cocaine?

Answer 19

Chattiness, euphoria, enhanced mental capabilities, feeling of alertness, energetic and physically strong
- increased confidence

Question 20

What are some of adverse affects of cocaine?

Answer 20

• tachycardia- cardiac arryth and coronary/cerebral thrombosis
• vasoconstriction
• increased BP- stroke out
• hyperthermia
• teratogenic- small brain and neuro/limb mutations

Overdose: tremors/convulsions
respiratory and vasomotor depression
- no clear withdrawal syndrome

Question 21

What is the MOA of methylxanthines?

Answer 21

inhibits phosphodiesterase to increase cAMP

adenosine receptor antagonist

Question 22

What are the main compounds found in Methylxanthines?

Answer 22

Caffeine and theophylline

- These are found in Tea, coffee and cocoa

Question 23

What are the clinical uses of methylxanthines?

Answer 23

Cardiac stimulation in CHF
Paroxysmal dyspnea in LHF 
analeptic
bronchial asthma
migraines 
students and working class