CNS Stimulants/Drugs of Abuse
Stimulants:
Methylxanthines – can cross the placenta; also increase
HR and CO; may produce cardiac
arrhythmias!
Nicotine – also increases BP and HR
Amphetamines – also cause appetite suppression and
insomnia; promote dopamine release; mainly used
to treat narcolepsy, and ‘hyperkinetic syndrome’
in children. Those used as anorexiants include:
Diethylpropion, Fenfluramine, Phentermine,
Phendimetrazine.
*adverse effects include: tachycardia, increased vagal
tone, hypertension, and cardiac arrhythmias
Cocaine
Abused drugs, by class:
CNS depressants: Alcohol
Barbiturates
CNS stimulants: Caffeine
Nicotine
Cocaine
Amphetamines
Hallucinogens: LSD
Mescaline
Psilocybin
Ketamine
Phencyclidine (PCP)
“designer drugs”
Inhalants: Nitrous oxide
Ether
Chloroform
organic nitrites
industrial solvents (turpentine)
aerosols/propellants
Antiepileptics
Main Drugs for Grand Mal and Partial Seizures:
Hydantoins – Phenytoin; less sedating than the ‘barbs, this
is the drug of choice for Grand Mal seizures
Barbiturates – Phenobarbital (not used for partials)
Primidone (active metabolites)
Iminostilbene – Carbamazepine (Tegratol); induces
microsomal enzymes
* phenytoin competes with antiinflammatory agents and
some hypnotics for plasma protein binding
Other Grand Mal and Partial Drugs:
Clonazepam
Diazepam
Lorazepam
Valproic acid
Vigabatrin – inhibits GABA transaminase
Gabapentin – new; can be use with other anitepileptics
Main Drugs for Petit Mal Seizures:
Succinimides – Ethosuximide; only administered orally
Carboxylic acids – Valproic acid
Benzodiazepines – Clonazepam; tolerance develops in
a few months, so this is not used for
long-term therapy
Oxazolidinediones – Trimethadone; sedation and
hemeralopia are the most common
side-effects encountered
Others – Acetazolamide; tolerance develops in a few
weeks!
Main Drugs for Status Epilepticus:
Diazepam
Lorazepam
Phenobarbital
Drugs for Parkinson’s & Movement Disorders
Parkinsonism:
Dopamine agonists:
Carbidopa (Lodosyn) – blocks amino acid
decarboxylase in the periphery (allows in
plasma levels of levodopa)
Levodopa (L-dopa)
Carbidopa/l-dopa (Sinemet)
Anticholinergics:
Benztropine (Cogentin)
Biperiden
Ethopropazine (Parsidol)
Orphenadrine (Disipal)
Procyclidine
Trihexyphenidyl (Artane)
Antihistamines/diphenhydramine – used for the potent
anticholinergic activities
Others:
Amantidine (Symmetrel) – can cause livido reticularis
(i.e.. discolored spots on the skin)
Seligeline (Deprenyl) – irreversible inhibitor of MAO-B
Bromocriptine – D2 receptor agonist
Pergolide – D2 receptor agonist
Lisuride – D2 receptor agonist
Spasmolytics:
Baclofen – is a GABA receptor agonist; primarily used to
treat spinal cord injuries/diseases and multiple
sclerosis; it is not metabolized before excretion
Dantrolene (Dantrium) – decreases Ca2+ release from the
sarcoplasmic reticulum; used in the treatment of
paralysis, hemiparalysis, cerebral palsy, and
multiple sclerosis
Diazepam (Vallium)
* antipsychotics and dopamine depleting agents (i.e.
reserpine) block the effect of L-dopa
* tachyphylaxis may occur with amantadine treatment