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Thereare four categories of drugs that are considered to have stimulant properties:
- Central Sympathomimetic Agents (Psychomotor Stimulants)
a group of potent and relatively nonselective CNS stimulants.
obsolete, but still valuable in determine hownew drugs act.
- Pentylenetetrazole (BN)
More selective and have use in narcolepsy and respiratory stimulant
- Modafinil (BN)
- Doxapram (BN)
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Drug is obsolete medically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.
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.
Doxapram HCl (BN)
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.
Caffeine (give the sources)
A dosage of _ to _ mg of caffeine acts as a cortical stimulant and facilitates clear thinking and wakefulness.
85 to 250
Have valuable bronchodilating properties in asthma.
Theophylline (give the source)
Classified as a xanthine alkaloid
Theobromine is formerly known as:
Chemical formula of theobromine
Theobromine is derived from :
Theobroma, the name of the genus of the cacao tree.
Psychomotor Stimulant or :
Central Sympathomimetic agents
-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.
- Dextroamphetamine Sulfate and
- Dextroamphetamine Phosphate (BN)
NOTE: The phosphate (more water-soluble salt); preferred if parenteral administration is required.
N-methyl analog of dextroamphetamine.More marked central and less peripheral action than dextroamphetamine.
Very high abuse potential. Its salts are known as “speed.”
- Methamphetamine Hydrochloride (BN) or
- 1-phenyl-2-methylaminopropane hydrochloride
Compound is used as an appetite suppressant and is a schedule IV agent.
-less abuse potential than dextroamphetamine.
- Phentermine Ion-Exchange Resin and
- Phentermine Hydrochloride
- NOTE: Resin preparation (Ionamin)- slow release product; Hydrochloride (Wilpower)
Has anorexiant properties
Benzephetamine Hydrochloride (BN)
-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.
Fenfluramine Hydrochloride (BN)
Considered an effective anorexiant that is less abuse prone than amphetamine.
Phendimetrazine Tartrate (BN)
-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:
- DIMETHYL Compounds(sedative,Higher 5-HT to norepinephrine reuptake block ratios, anticholinergic properties)
- MONOMETHYL COMPOUNDS (Selective Norepinephrine reuptake,stimulatory)
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.
Imipramine Hydrochloride (BN?)
Selective norepinephrine reuptake inhibitor.
Desipramine Hydrochloride (BN?(2))
Used in OCD (obsessive compulsive disorders)
Clomipramine Hydrochloride (BN?)
One of the most anticholinergic and sedative of the tricyclic antidepressants.
Treat mental/mood problems such as depression.
Amitriptyline Hydrochloride (BN?)
BN of Trimipramine Maleate (TCA drug)
Norepinephrine and 5-HT reuptake blocker withsignificant anticholinergic and sedative properties
Doxepin Hydrochloride (BN(2))
Maprotiline Hydrochloride (BN?)
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)
- Fluoxetine (BN)
- Paroxetine (BN)
- Setraline (BN)
- Citalopram (BN)
It is claimed to be superior to fluoxetine in severe depression
Reboxetine (RR & SS)
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.
- Nefazodone (Serzone),
- Trazadone (Desyrel)
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)
- Bupropion (Wellbutrin)
- Duloxetine (Cymbalta)
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.
- threohydrobupropion and
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:
1ᵝ -Arylamino Hallucinogens
A property of the 1B-arylamino hallucinogens.
alteration of the perception of stimuli.
can produce anxiety, fear, panic, frank hallucinations, and additional symptoms that may be found in a psychosis.
- Accordingly, they are classed as hallucinogens
- and psychotomimetics.
1ᵝ -Arylamino Hallucinogens can be subgrouped into:
- those that possess an indolethylamine moiety,
- those that possess a phenylethyl- amine moiety, and
- those with both
- Psilocybin and Psilocin
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: ____)
Psilocybin occurs in
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)
- (+)-Lysergic Acid Diethylamide
- (DOM),(MDA), (DMDA; ECSTASY)
It has marked effects on serotoninergic and
dopaminergic neurons. Both an indolethylamine group and a phenylethylamine group
(+)-Lysergic Acid Diethylamide
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.
is a euphoriant–stimulant, psychotomimetic, and drug of abuse. At low doses, it produces feelings of well-being, decreased
fatigue, and increased alertness
∆1-Tetrahydrocannabinol or ∆⁹-THC
Two receptors for THC have been discovered.
- The relevant receptor for CNS actions is CB1.
- CB2 occurs in immune tissues
involved in maintaining food intake and in other
Endocannabinoids (regulated by leptin)
Other natural cannabinoids : (2)
- arachidonic acid 2-glycerol ester and
- 2-arachidonyl glycerol ether