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CNS STIMULANTS

CLASSIFICATION INDICATIONS DRUG ACTION

Amphetamines treatment of attention deficit hyperactivity The exact mechanism of amphetamines as a class is not known.
disorder (ADHD) Dextroamphetamine acts by preventing reuptake, increasing release, and
Dextroamphetamine sulfate stimulating reverse-transport of dopamine in synaptic clefts in the striatum. Newer
(Adderall, Dexedrine, Mydayis, evidence shows amphetamines may also alter the number of dopamine
Procentra, Zenzedi) transporters in synaptic clefts.

Anorexiants used to help manage weight in obese or Contrave is combination of naltrexone, an opioid antagonist, and bupropion, an
overweight adults with weight-related inhibitor of the neuronal reuptake of dopamine and norepinephrine. Nonclinical
Contrave (bupropion and medical problems. This medicine is used studies suggest that naltrexone and bupropion have effects on two separate areas
naltrexone) together with diet and exercise. of the brain involved in the regulation of food intake: the hypothalamus (appetite
regulatory center) and the mesolimbic dopamine circuit (reward system). The exact
neurochemical effects of Contrave leading to weight loss are not fully understood. 

Analeptics used to treat conditions such as The exact mechanism of action is unclear, although in vitro studies have shown it to
obstructive sleep apnea, hypopnea inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and
Modafinil (Provigil) syndrome (OSAHS), narcolepsy, and shift lead to an increase in extracellular dopamine. Modafinil activates glutamatergic
work sleep disorder. circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse
than other stimulants due to the absence of any significant euphoric or pleasurable
Off-label: may reduce fatigue in multiple effects. It is possible that modafinil acts by a synergistic combination of
sclerosis (MS) patients and depression. mechanisms including direct inhibition of dopamine reuptake, indirect inhibition of
noradrenalin reuptake in the VLPO and orexin activation. Modafinil has partial alpha
1B-adrenergic agonist effects by directly stimulating the receptors.
CNS DEPRESSANTS

CLASSIFICATION INDICATIONS DRUG ACTION

oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-


Sedative-hypnotics aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory
(Anxiolytics) Oxazepam is indicated for the management neurotransmitter receptors in the mammalian brain. GABA(A) receptors are a
of anxiety disorders and for the short-term component of GABA-gated ionotropic chloride channels that produce inhibitory
Oxazepam (Oxpam, Serax) relief of symptoms of anxiety.It may also be postsynaptic potentials - following activation by GABA, the channel undergoes a
used in the management of alcohol conformational change that allows the passage of chloride ions through the
withdrawal symptoms. channel. The inhibitory potentials produced by GABA neurotransmission play an
integral role in the suppression and control of epileptiform nerve firing such as that
seen in epilepsy, which makes the GABA system a desirable target in the
treatment of epilepsy.

Analgesics For the relief of moderate to severe pain. The exact mechanism of action is unknown, but is believed to interact with an
opiate receptor site in the CNS (probably in or associated with the limbic system).
Nalbuphine The opiate antagonistic effect may result from competitive inhibition at the opiate
receptor, but may also be a result of other mechanisms. Nalbuphine is thought
primarily to be a kappa agonist. It is also a partial mu antagonist analgesic, with
some binding to the delta receptor and minimal agonist activity at the sigma
receptor.

Anticonvulsants Used in patients over 12 years old for the The exact mechanism of action of perampanel in seizures is not yet determined,
treatment of partial-onset seizures that may but it is known that perampanel decreases neuronal excitation by non-competitive
Perampanel (Fycompa) or may not occur with generalized seizures. ihibition of the AMPA receptor.

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