CNS Stimulants

Thereare four categories of drugs that are considered to have stimulant properties:

a group of potent and relatively nonselective CNS stimulants.

obsolete, but still valuable in determine hownew drugs act.

More selective and have use in narcolepsy and respiratory stimulant

MOA: Intefere with the inhibitory effects of y-aminobutyric acid (GABA) at the level of the GABAa receptor's chloride channel.
Drug is obsolete medically

Used  in conjunction with the electroencephalograph to help locate epileptic foci. Used as a laboratory tool in determining potencies of potential anticonvulsant drugs in experimental animals

Used in overall wakefulness-promoting properties similar to those of central sympathomimetics.Atypical a-norepinephrine (NE) receptor stimulant and is used to treat daytime sleepiness in narcolepsy patients.
SE: nervousness, anxiety, andinsomnia.
Route: Oral

Has an obscure molecular mechanismof action.
MOA: Stimulates respiration by action on peripheral carotid chemoreceptors.
Use: Respiratory stimulant post-anesthetically, after CNSdepressant drug overdose, in chronic obstructive pulmonary disease, and in the apneas.
Route: IV; not given to neonates because of benzyl alcohol.

Naturally occurring Methylxanthines are:

is a widely used CNS stimulantit promotes an ability to concentrate on the task at hand, and lessens fatigue.may be used in treating poisoning from CNS-depressant drugs, although it is not a preferred drug.

A dosage of _ to _ mg of caffeine acts as a cortical stimulant and facilitates clear thinking and wakefulness.

Have valuable bronchodilating properties in asthma.

Classified as a xanthine alkaloid

Theobromine is formerly known as:

Chemical formula of theobromine

Theobromine is derived from :

Psychomotor Stimulant or :

-exert an anorexiant effect.
-more resistant to metabolism, more non-polar.
-able to cross the blood-brain barrier.
-increase the ratio of central peripheral activity.

Chemical Name and Brand name of Amphetamine Sulfate

The dextrorotatory isomer has the (S) configuration and fewer cardiovascular effects than the levorotatory (R)-isomer.MOA: Release of NE from the mobile pool of the nerve terminal.

N-methyl analog of dextroamphetamine.More marked central and less peripheral action than dextroamphetamine.
Very high abuse potential. Its salts are known as “speed.”

Compound is used as an appetite suppressant and is a schedule IV agent.
-less abuse potential than dextroamphetamine.

Has anorexiant properties

-Fewer sympathomimetic, cardiovascular and CNS-stimulatory effects than amphetamine.
-an anorexiant agent.
-can be used for treatment of obesity in patients with hypertension and cardiovascular disease.

(unique in this group of drugs)-tends to produce sedation rather than excitation.

Considered an effective anorexiant that is less abuse prone than amphetamine.

-an uptake inhibitor of NE and 5-HT-An antidepressant and an anorexiant drug.

Brand name of Methylphenidate Hydrochloride, a CSA.

The tricyclic antidepressants are structurally related to each other and possess related biological properties that can be summarized as characteristics of the group as:

are extremely lipophilic and very highly tissue bound outside the CNS.  Because they have anticholinergic and noradrenergic effects, both  central and peripheral side effects are often unpleasant and sometimes dangerous.

Lead compound of TCA.Selective transport inhibitor to treat depression. Treatment of night time bed wetting in children. May improve your mood, sleep, appetite, and energy level and may help restore your interest in daily living.

Selective norepinephrine reuptake inhibitor.

Used in OCD (obsessive compulsive disorders)

One of the most anticholinergic and sedative of the tricyclic antidepressants.
Treat mental/mood problems such as depression.

BN of Trimipramine Maleate (TCA drug)

Norepinephrine and 5-HT reuptake blocker withsignificant anticholinergic and sedative properties

“tetracyclic” depressant
-SNERI

8-hydroxy metabolite is active as antidepressant and D2 receptor blocker

differ from the tricyclics, in that the tricyclic system has been taken  apart in the center.  This abolishes the center ring, and one ring  is moved slightly forward from the tricyclic “all-in-a-row” arrangement

this diminishes unpleasant CNS effects and in- creases cardiovascular safety.

Therapy for 2 weeks or more is required for the anti-depressant effect. S-isomer moreselective for SERT.

Anti-depressant and anxiolytic.

The Cl substituents also predict tropism for a5-HT system.

A racemic mixture and is very SERT selective.

SSRIs : (4)

SNERIs: (1)
It is claimed to be superior to fluoxetine in severe depression

NEWER (NONTRICYCLIC) NONSELECTIVE 5-HT AND NOREPINEPHRINE REUPTAKE INHIBITORS : (1)is an effective antidepressant. ___ is a serotonin–norepinephrine reuptakeinhibitor (SNRI).

SELECTIVE SEROTONINERGIC REUPTAKE INHIBITORS AND 5-HT2A ANTAGONISTS: (2)The structures of these two compounds derivefrom those of the fluorobutyrophenone antipsychotics.

not as an antidepressant. A 100-mg dose can be used as a sedative–hypnotic.

produces better sleep hygiene than does trazodone, which is a rapid eye movement (REM)-suppressing compound.

5-HT₁ₐ AGONISTS AND PARTIAL AGONISTS: (1)
has anxiolytic and antidepressant activities and is a partial 5-HT₁ₐ agonist. Its anxiolytic activity is reportedly caused by its ability to diminish 5-HT release (via 5-HT₁ₐ agonism).

α2 ANTAGONISTS: (1)
Its parent, mianserin, was long known to be an
antidepressant. It is reported to be faster acting and more potent than certain SSRIs

MISCELLANEOUS ANTIDEPRESSANTS : (2)

It is considered complex and reportedly involves a block of DA re- uptake via the dopamine transporter (DAT), but the overall
antidepressant action is noradrenergic

In Bupropion, reduction of the keto group also occurs, yielding _____ and ____ . Both of these metabolites are also active.

It is a newer antidepressant. It is largely like venlafaxine, which is a selective norepinephrine reuptake inhibitor. It is a treatment for depression, anxiety, muscle and bone aches.

MISCELLANEOUS CNS-ACTING DRUGS:

A property of the 1B-arylamino hallucinogens.

can produce anxiety, fear, panic, frank hallucinations, and additional symptoms that may be found in a psychosis.

1ᵝ -Arylamino Hallucinogens can be subgrouped into:

INDOLETHYLAMINES: (2)

It is a very weak hallucinogen, active only by inhalation or injection, with a short duration of action. It possesses pronounced sympathomimetic (NE) side effects.

is the phosphoric acid ester of psilocin and
appears to be converted to psilocin as the active species in vivo.

Psilocybin occurs in

2-PHENYLETHYLAMINES

It is a much- studied hallucinogen with many complex effects on the CNS. It occurs in the peyote cactus. The oral dose required for its hallucinogenic effects is very high, as much as 500 mg of the sulfate salt.

Mescaline occurs in :

AN AGENT POSSESSING BOTH AN INDOLETHYLAMINE AND A PHENYLETHYLAMINE MOIETY (2)

It has marked effects on serotoninergic and
dopaminergic neurons. Both an indolethylamine group and a phenylethylamine group

(DMDA; Ecstasy).

DISSOCIATIVE AGENTS (1)

It was introduced as a dissociative anesthetic
for animals.In humans, PCP produces a sense of intoxication, hallucinogenic experiences not unlike those produced by the anticholinergic hallucinogens, and often, amnesia.

EUPHORIANT-STIMULANT

is a euphoriant–stimulant, psychotomimetic, and drug of abuse. At low doses, it produces feelings of well-being, decreased
fatigue, and increased alertness

DEPRESSANT-INTOXICANT

Two receptors for THC have been discovered.

involved in maintaining food intake and in other
behaviors.

Other natural cannabinoids : (2)