stimulants Flashcards
What are some stimulant drugs?
- Amphetamines (benzedrine)
- Cocaine
- Ritaline (Methylphenidate)
- MDMA (Ecstasy, molly)
- Bath Salts (methlenedioxypyrovalerone, Mephedrone)
- Xanthines like caffeine and theophylline
What is a sympathomimetic?
A drug that acts as an agonist of the sympathetic NS
What are some examples of amphetamines?
Adderall
speed
crystal meth
What are some effects of amphetamines?
Excitement Euphoria Increase motor activity Some increased cognitive function Insomnia anorexia and adverse actions are anxiety, irritability and restlessness
What is the mechanism of action of Amphetamines?
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
What is VMAT-2?
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
What is the clinical use of amphetamines?
Treatment of ADHD
Narcolepsy
Past: weight loss and fatigue but not recommended
What are some chronic adverse effects of amphetamines?
Amphetamine psychosis- which resembles schizophrenic attack with hallucinations, paranoia and aggressive behavior.
Is there dependence on amphetamines?
Yes,
Strong psychological dependence: Insistent memory of euphoria
However, no clear cut withdrawal syndrome
What is the mechanism of action of Ritalin?
Profound elevation of NE and DA
- Via inhibits NET and DAT transporters
- but does not enter cell to facilitate release of NT inside cell
Other facts about Ritalin?
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
What is Ritalin used to treat?
ADHD
What is the mechanism of action of Modafinil?
Increases DA Levels in striatum and nucleus accumbens through inhibition of DAT’s
- also increased 5-HT, Glutamate and histamine
- inhibits GABA release
What does Modafinil used to treat?
Sleep apnea
Narcolepsy
shift work disorders
ADHD in adults
What is the mechanism of action of MDMA?
Inhibits monoamine transporters, prinicpially 5-HT transporters. SERT’s
- also released Serotonin
- SSRI
- inhibits DAT’s and NET’s
Is MDMA addictive and what can it be used for?
No
Treatment of PTSD and depression
Sudden death or illness can happen when taking MDMA, this is due to what?
acute hyperthermia
excessive water consumption- which causes hyponatremia
- because 5HT is important in thermoregulation
What is the mechanism of action of Cocaine?
Binds too and inhibits NET, DAT and SERT’s
- psychomotor stimulant
- also used as a local anesthetic
What are some of the effects of cocaine?
Chattiness, euphoria, enhanced mental capabilities, feeling of alertness, energetic and physically strong
- increased confidence
What are some of adverse affects of cocaine?
- 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
What is the MOA of methylxanthines?
inhibits phosphodiesterase to increase cAMP
adenosine receptor antagonist
What are the main compounds found in Methylxanthines?
Caffeine and theophylline
- These are found in Tea, coffee and cocoa
What are the clinical uses of methylxanthines?
Cardiac stimulation in CHF Paroxysmal dyspnea in LHF analeptic bronchial asthma migraines students and working class
