CNS STIMULANT - BASIC NEUROPHARMACOLOGY

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 Methylxanthines

Theophylline, Caffeine, Cocaine...

MOA 

Inhibit PhosphodiEsterase enzymes..Increase cAMP ....Block Adenosine receptor...Alter intracellular Ca++..Increase Ca++ in Brain..decrease Ca++ in smooth muscles

Actions

increased mental alertness. +Ve ionotropic & chronotropic effect on heart.. ..

Diuretic action...Stimulate secretions... contraindicated in Peptic ulcer..

T.E

in Asthma.... in Headache...

S.E

 Insomnia.... cardiac arrhythmia...

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Nicotine

 second most abused drug.

MOA

 cause ganglionic stimulation by depolarization..At high dose blockade of ganglia

Actions

 Euphoria...arousal...respiratory paralysis...Vasoconstriction.... increaase B.P....Appetite suppressant

S.E

 Diarrhea, tachycardia, withdrawal characterized by irritability, anxiety, difficulty in conc. Headache, insomnia...

Bupropion used to reduce craving for smoking

Varencilline

 Partial agonist at neural nicotinic Ach receptor in CNS...used as Adjunct in smoking cessation therapy.

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Cocaine

 highly addictive drug...Schedule ll drug by U.S Drug Enforcement Agency...

MOA

block reuptake of MonoAmine...prolong CNS effect intense EUPHORIA... Fight & Flight syndrome...hyperthermia

T.E

local anaesthetic...by blocking Na+ channel ...cause vasoconstriction

Benzoylecqonine 

 metabolite of cocaine...detection of this substance in urine

S.E

Anxiety...hypertesion...tachycardia...depression...seizure

Cocaethylene

metabolite of cocaine and ethanol casue cardiac toxicity

Amphetamine

 sympathetic amine.

MOA

increase release of Catecholamine & inhibit MOA enzyme

Actions

Euphoria, Dizziness, Hyperthermia, insomnia

T.E

in Narcolepsy (uncontrollable bouts of sleep during day) ...modafinil used.... Attention Deficit Hyperactive Syndrome, methylphenidate OR lisdexamfetamine used

S.E

Amphetamine psychosis (associated with Schizophrenia)...suicidal tendency..

headache,hypertension ...contra in hyperthyroidism, hypertension, CVS disorder

Methylphenidate

similar mechanism to Amphetamine...Schedule lldrug...one of the most prescribed to children for ADHD...Ritalinic acid metabolite..

Contraindicated in Glaucoma...S.E: seizure, Abdominal pain, nausea

Central Nervous System (CNS) Stimulants Amphetamines (including ecstasy or methylenedioxymetamphetamine) Armodafinil. Atomoxetine. Cocaine. Methylphenidate. Modafinil.


Hallucinogens

Ability to produce perceptual state of dreams, bright vision, colorful changes in environment, impair decision making ability..

Lysergic acid diethylamide LSD= bind to 5-HT2 receptor...stimulate limbic & cortex in

CNS...induce hallucination with brilliant color..tolerance & physical dependence

S.E

 hyper-reflexia, muscle weakness,

TetraHydroCannabinol(THC)

contained in Marijuana..available as Dronabinol..

Neuromodulator

MOA

CB1 RECEPTOR..excitation of post-synaptic neurons cause depolarization..influx

of Ca++...stimulate Endo-cannabinoid...endocannabinoid inhibit release GABA..

T.E

 increase appetite..suppres emesis..Euphora

S.E

redning of conjunctiva

Droanbinol

appetite stimulant in Pt. with AIDS

Rimonabant

in treatment of obesity by suppressing appetite

Phencyclidine

PCP/Angel dust..

MOA

block glutamate activated NMDA...inhibit reutake of catecholamine..

T.E

 in Dissoiciative Anaesthesia (without lossof consciousness) ..Analogue of

Ketamine ...numbnesss in extremeties...bizarre behavior

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