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173 Cards in this Set
- Front
- Back
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Thiopental (Pentothal)
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Barbiturate - NE downer
ultra sort acting Tx= anesthesia inducer (-) GI spasms |
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Thioridazine (Mellaril)
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Phenothiazine
Clasical Antipsychotic block D2, A-adrenergic, histamine receptors Low potency High anticholinergic SE= Low extrapyramidal High adrenergic blockade |
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Dantrolene (Dantrium)
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Muscle relaxant
SER calcium channel action Direct muscle action Tx= malignant hyperthermia, neuroleptic malignant syndrome |
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Phenelzine (Nardil)
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MAOI - upper
irreversibly (-)MAO-A^B Tx= anxiety disorder, atypical depression, bulimia, refractory depression, social phobia SE= Serotonin Syndrome |
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Thiothixene (Navane)
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Antipsychotic - DA downer
like-phenothiazine |
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Haloperidol (haldol)
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Butyrophenone
Classical Anti-psychotic Selective (-)D2 - DA downer No ACh effect Oral^IV HIGH potency Tx= alcohol withdrawal, halucinations, acute psychosis, tourette's SE= Neuroleptic Syndrome, hyperprolactemia Low (-)adrenergic High EPS |
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9 major acting neurotransmitters in the CNS
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Acetycholine (ACh)
Nor-epinephrine/adrenaline Dopamine Serotonin GABA Glutamate Glycine Neuropeptides Cannaboids |
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ACh funtion in CNS neurotransmission
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modulation of CNS to rest and digest
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Cholinergic pathway in CNS
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Neucleus basalis of Meynert
and septum --> cerebral cortex and hippocampus (degenerates > Alzheimer's) |
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Cholinergic receptors
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M1> activated PLC(IP3^DAG)=excite
M2> hippocampus^cortex =inhibitory M4> Tx of schizophrenia |
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Cholinergic drugs w/direct effects
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Nicotine
Muscarinic receptor antagonist cholinesterase inhibitor |
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Serotonin (5-HT) function in CNS neurotransmission
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Modulates alertnes
(+)5-HT = vigilance (-)5-HT = sleep |
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Serotonergic pathway in CNS
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Raphe nucleus --> limbic system^cerebral cortex
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Serotonergic receptors
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[5-HT]
1a> (-) cAMP levels (inh) 2a> (+) IP3^DAG (exc) 3> cation conductance (exc) 4> K conductance (exc) |
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Noradrenergic function in CNS neurotransmission
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Modulation of CNS to activate movement
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Noradrenergic pathways in CNS
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descending noradrenergic --> pain modulation
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Noradrenergic receptors
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a1> (+) PLC -> + IP3^DAG (exc)
a2> presynaptic - cAMP (inh) b1> (+) cAMP b2> (+) cAMP |
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Dopamine function in CNS
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Movement coordination
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Dopaminergic pathway in CNS
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ventral tegmental>nucleus accumbens^prefrontal cortex
Nigro-striatal system -> movement |
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Dopaminergic receptors
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D1> (+) cAMP (inh)
D2> (-) Ca influx,cAMP (inh) |
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GABA function in CNS
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(-)Responsiveness to stimulus
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GABA receptors
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Major inhibitory
A> (+) Cl conductance (inh) B> (-) Ca conductance (inh) |
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Glutamate function in CNS
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(+)Responsiveness to stimulus
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Glutamate receptors
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Modulate neurotransmission
NMDA = ionotropic (+) = learning^memory Kainite = ionotropic (+) = NT release AMPA = ionotropic (+) = (+) neurotransmission mGluR = metabotropic (+) = (+) neurosynchrony |
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Glycine function in CNS
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Memory and pain modulation
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Glycine receptors
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(+) Cl conductance (inh)
blocked by strychnine modulators of NMDA> strychnine insensitive |
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Neuropeptide function in CNS
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Modulation of perceptions
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Opioid neuropeptide receptors
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B-endorphin> (+) mu receptor
Enkephalin> (+) delta receptor Dynorphin> (+) kappa receptor |
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Substance P neuropeptide
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(exc) in sensory pathways
unmyelinated sensory fibers> (+) w/painful stimulation |
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Capsaicin neuropeptide
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(-) Substance P release> numbness to pain
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Cannabinoid functions in CNS
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memory, cognition, perception, neurotransmitter modulator
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Cannabinoid receptors
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D9-THC
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Barbiturate drugs
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Phenobarbital
Thiopental |
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Benzodiazepines drugs
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Diazepam
Chlordiazepoxide Flurazepam Midazolam Temazepam Triazolam Alprazolam Lorazepam |
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Sedative-Hypnotic and Anxiolitic Drug function
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(+) GABAa receptor modulator
Sx= depression of CNS |
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Barbiturate drug function
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(+) DoA of GABA
Sx= hypnosis, surgical anesthesia |
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Barbiturates drug effects
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Low margin of safety
(-) repisratory drive Abuse potential (+) effect w/ alcohol |
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Barbiturates pharmacokenetics
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Enter CNS
Liver (+) CytP450 |
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Phenobarbital (Luminal)
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barbiturate
long acting anticonvulsant |
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Barbiturate SE
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Drug SE=
depression>drowsiness vertigo^impaired judgement (-) REM sleep n/v/d paradoxical excitement respiratory depression dependance (+) withdrawal |
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Barbiturate withdrawal
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Sx of drug withdrawals=
restlessness, anxiety, weakness, orthostatic hypotension, hypereflexia, seizure |
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Barbiturate CI
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absolute contraindication>porphyria
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Benzodiazepine SE
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(+) GABA binding only w/GABA
Sx= CNS depression drowsiness hypnosis muscle relaxation anticonvulsant |
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Benzodiazepine pharmacokinetics
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oral
IV for seizure emergencies^pre-anesthesia rapid uptake redistribution |
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Desmethyldiazepam
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Metabolite from=
diazepam chlordiazepoxide |
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Oxazepam (serax)
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Benzodiazapine
Short-acting Tx= alcohol^barbiturate withdrawal w/ liver damage Metabolite= desmethyldiazepam |
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Flurazepam (Dalmane)
Temazepam (Restirol) |
benzodiazepines
long acting hypnotics Tx= Difficulty staying asleep SE= drug hangover |
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Alprazolam (Xanax)
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benzodiazepine
Tx= antidepressant, anxiolytic, panic disorder |
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Triazolam (Halcion)
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benzodiazepine
short acting hypnotic Tx= Difficulty falling asleep SE= Psychosis |
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Cloazepam (Klonipin)
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Benzodiazepam
Tx= Prevention of abscent seizures |
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Diazepam (Valium)
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Benzodiazepam - downer
(+)GABA-A receptors of spinal cord long acting Tx= drug psychosis, alcohol^barbiturate withdrawal, nerve pain, IV for status epilepticus, acute muscle spasm DI= Cimetidine (Tagamet) (-) metabolism |
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Lorazepam (Ativan)
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benzodiazepam
Tx= IV for status epilepticus |
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Chlordiazepoxide (Librium)
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benzodiazepam
long acting Tx= alcohol^barbiturate withdrawal |
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Benzodiazepine SE
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Drug SE=
CNS depression, develop tolerance, impaired learning/memory in children, memory loss/ confusion, blurred vision, halucinations, paradoxical excitement, hyperactivity/ aggression, withdrawal |
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Benzodiazepine CI
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Drug CI=
pregnancy children sleep apnea |
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Benzodiazepine withdrawal Sx
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withdrawal Sx=
anxiety insomnia muscle weakness tremor hyperalgesia n/v/d convulsions/ seizures halucinations |
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Flumazenil (Romazicon)
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Benzodiazepine antagonist
only IV, push slowly Tx= benzodiazepine overdose SE= trigger withdrawal seizures |
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Zolpidem (Ambien)
Zaleplon (Sonata) |
Sedative-Hypnotic
binds BZ1 receptor Very strong and rapid sedative Tx= Short term insomnia SE= drowsiness, dizziness, Blackouts, amnesia |
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Eszopiclone (Lunesta)
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Sedative-Hypnotic
binds all 3 BZ receptors Very strong and rapid sedative Tx= Long term insomnia SE= drowsiness, dizziness, Blackouts, amnesia, withdrawal |
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Ramelteon (Rozerem)
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Sedative-Hypnotic
Melatonin1 receptor agonist Tx= Difficulty falling asleep, (+) sleep time CI= Not for severe liver disease DI= Rifampin (+) metabolism HIV protease inhibitors, -conazoles, fluvoxamine (-) metabolism |
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Antihistamines w/ Sedative properties
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Diphenhydramine (Benadryl)
Promethazine (Phenergan) Hydroxyzine (Vistaril) BBW = severe CNS depression in children |
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Chloral hydrate (Noctec, Somnos)
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Conscious Sedative
active metabolite = trichloroethanol cheap Tx= Pediatric dental procedures SE= GI, allergy, arrhythmias, n/v, unpleasant taste, repiratory/vasomotor depression |
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Buspirone (BuSpar)
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Anxiolytic in addiction/autism
5-HT1A receptor partial agonist (-) serotonin release from dorsal raphe nuclei SE= HA, drowsiness, n/v, restlessness, (-) BP DI= MAOI (Serotonin Syndrome) |
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Kava
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OTC herbal sedative
SE= tingling in mouth, GI, skin rash CI= liver toxicity, pregnancy |
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Valerian
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Herbal Sedative
w/ chamomile CI= liver toxicity, pregnancy |
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Alcohol neurotransmitor activity
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augment GABA-A receptor
(-) glutamate on NMDA receptor Chronic use = down-regulate GABA receptor up-regulate NMDA receptor |
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Alcohol pharmakokinetics
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absorbed in stomach/small intestines
slowed w/ food metabolized in GI by alcohol dehydrogenase metabolism speed= females<males crosses placenta/blood-brain barrier levels function of body water |
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Alcohol metabolism
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In GI tract and liver by a dehydrogenase (NAD+)
Zero order kinetics 8-10 g/hour - NAD+ -> + lactate, acetylCoA, Trig, ketones ->lactic acidosis (-) TCA cycle (+)CytP450 CyP2E1 |
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Alcohol effects
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CNS depression of hibition, anxiety, alertness, motor function
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Alcohol toxicity
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Drug SE=
emesis, stupor, coma, respiratory depression, metabolic disturbance, cutaneuos vasodilation (hypothermia) |
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Alcohol hangover
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Build-up of acetylaldehyde
dehydration withdrawal |
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Chronic Alcohol Consumption SE
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Drug SE=
malnutrition (folate^thiamine) Gastritis^pancreatitis Esophageal/Duodenal lesions Hepatotoxicity w/ fatty liver and Hep B or C risk Liver Cancer Cardiomyopathy |
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Fetal Alcohol Syndrome
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Syndrome characterized by SSx=
microcephaly, flattened face, joint abnormalities mental redartation, poor coordination, immune system impaired |
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Korsakoff's psychosis
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Characterized by SSx=
Chronic disabling memory loss Alcoholism |
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Wernicke encephalopathy
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Characterized by SSx=
paralysis of eye muscles, ataxia, confusion |
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Alcohol withdrawal
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Withdrawal characterized by SSx=
Anxiety, irritability, fear, hallucinations, delirium, tremors, insomnia, nightmares tonic-clonic seizures, arrhythmias, (+) BP |
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Naltrexone (Revia, Vivitrol)
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Opiod receptor antagonist
blocks released beta-endorphins short acting Tx= Alcoholism by reducing craving SE= nausea, liver damage, reduced use of opiods for therapy |
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Nalmefene (Revex)
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Opiod receptor antagonist
blocks released beta-endorphins long acting Tx= Alcoholism by reducing craving SE= nausea, reduced use of opiods therapy |
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Acamprosate (campral EC)
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GABA analogue
balances GABA^glutamate Tx= Alcoholism |
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Disulfaram (Antabuse)
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Blocks alcohol dehydrogenase
Causes acetaldehyde buildup w/ Alcohol SE= hives, tremor, HA, diziness, metalic taste, GI, peripheral neuropathies, ketosis |
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Disulfram (Antabuse)
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Long acting
Detorant w/ Alcohol SE= flushing, intense HA, nausea, confusion, syncope, vertigo, shock |
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Topiramate (Topamax)
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Anticonvulsant
Tx= Alcoholism by decreasing craving |
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Methanol poisoning
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Characterized by SSx=
visual disturbances, bradycardia, coma, seizures, acidosis, repiratory depression Tx= ethanol, Fomepizole (Antizol) |
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Ethylene Glycol poisoning
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Characterized by SSx=
transient CNS excitation to depression, metabolic acidosis Tx= ethanol, Fomepizole (Antizol) |
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Fomepizole (Antizol)
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Alcohol dehydrogenase inhibitor for ethylene glycol^methanol poisoning
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Fluoxetine (Prozac, Serafem)
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SSRI - upper
Long lasting active metabolite (+) CYP2D6 Tx= Depression, dysthymia, PMS (Serafem) DI= TCA, benzodiazepines, antipsycotics, opiods SE= HA, SIADH, insomnia, restlessness^agitation photosensitivity, GI, sexual dysfunction, Serotonin Syndrome |
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Paroxetine (Paxil)
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SSRI - upper
short acting Tx= OCD (DoC), anxiolytic, adult depression, premature ejaculation, hot flashes SE= anorexia, nausea, sedation, photosensitivity, GI, sexual dysfunction |
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Sertraline (Zoloft)
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SSRI
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Citalopram (Celexa)
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SSRI
faster OoA fewer side effects than fluoxetine^setraline |
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Escitalopram (Lexapro)
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SSRI
S-enantiomer of citalopram faster OoA fewer side effects than fluoxetine^setraline |
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Reserpine
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Drug that depletes NE and 5-HT
Use develops depression |
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Clomiparamine (Anafranil)
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Similar to SSRI
Tx= OCD |
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TCA mechanism
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(-) uptake of NE^5-HT
block muscarinic, alpha-adrenergic, histamine receptors |
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Imipramine (Tofranil)
Amitriptyline (Elavil) |
TCA tertiary - upper
active metabolites -> secondary TCA - long lasting Tx= depresion w/pain SE= Adrenergic blockade |
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Desipramine (Anafranil)
Nortriptyline (Pamelor) |
secondary TCA
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TCA SE
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Drug effect SSx=
Drowsiness^sedation -> histamine blockade memory^cognition impairment, ANS depression -> muscarinic blockade Analgesia, cardiac depression^Torsades de pointes^postural hypotension -> A1 adrenergic blockade, weight gain, decrease seizure threshold SIADH -> water intoxication Sexual dysfunction used w/ pregnancy |
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Imipramine (Tofranil)
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TCA tertiary - NE upper
Tx= standard efficacy in depression, enuresis, tyramine posoining |
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TCA withdrawal
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Withdrawal SSx=
Muscle aches, malaise |
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TCA overdose
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Overdose SSx=
Torsades de points, hypotension, seizures Tx= phenytoin, sodium bicarbonate^potassium chloride |
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Serotonin syndrome
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Syndrome characterized by SSx=
hyperpyrexia, convulsions, coma, muscle twitch, mydriasis, myoclonus, hyperreflexia DI= MAOI+SSRI/Meperidine (Demerol)/TCAs/dextromethorphan/SJW St. John's Wort+MAOI/SSRI/TCA/l-dopa/seregiline |
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MAOI mechanism
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MAO-A breaks down NE^5-HT
MAO-B breaks down DA |
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Hypertensive Crisis
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(+)Tyramine - NE upper
MAOI in GI w/ red wine, beer, cheese, sympathomimetic drugs SSx= intracranial bleed w/HTN |
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MAOI SE
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Drug SE SSx=
tremors, orthostatic hypotension, delayed ejaculation, skin rash, weight-gain, anticholenergic effects |
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Moclobemide (Aurorix)
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MAOI
reversible (MAO-A) decrease severe HTN Tx= postmenopausal hot flashes |
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SSRI mechanism
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inhibit serotonin reuptake
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Clomipramine (Anafranil)
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SSRI
Tx= OCD (DoC) |
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SSRI SE
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Drug SE=
n/v/d, constipation, weight loss (initial), weight gain (chronic), sexual dysfunction, photosensitivity, rash, HA |
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SSRI DI
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DI=
toxicity - TCA, phenytoin, beta/CC-blockers (-) efficacy - opiods bleeding - warfarin |
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Setraline (Zoloft)
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SSRI
more selective short acting less side effects Tx= depression |
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Venlafaxine (Effexor)
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Inhibitor of 5-HT and NE reuptake
metabolite= desvenlafaxine long acting Tx= depression w/ chronic pain syndrome SE= HTN, n/v, constipation, hyponatremia, SIADH |
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Desvenlafaxine (Pritiq)
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Inhibitor of 5-HT and NE reuptake
metabolite of venlafaxine long acting Tx= depression w/ chronic pain syndrome, hotflashes SE= HTN, n/v, constipation, hyponatremia, SIADH |
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Duloxetine (Cymbalta)
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Inhibits 5-HT^NE reuptake
greater efficacy Tx= depression w/ chronic pain syndrome SE= hepatotoxic, anticholinergic effect, sinus tachycardia |
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Bupropion (Wellbutrin, ER=Zyban)
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Selective (-)DA^NE reuptake - upper
Tx= smoking cessation, kids w/ADHD, alcoholism, neuropathic pain, SSRI combo SE= Lowest risk of sexual dysfunction, CNS stimulation, HA, nausea, weightloss, SEIZURES |
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Atomoxetine (Strattera)
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Non-stimulant CNS
Selective (-)NE reuptake Tx= ADHD SE= GI, insomnia, liver damage (rare), (+)BP |
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Maptrotiline (Ludiomil)
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NE reuptake inhibitor
Tx= ADHD (non-stimulant) SE= dose related seizures |
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Amoxapine (Ascendin)
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LOW potency Antipsychotic
TCA-like DA receptor antagonist Tx= depression w/ schizophrenia SE= Parkinsonian, amenorrhea, glactorrhea, tardive dyskinesia |
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Trazodone (Desyrel)
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partial 5-HT1A agonist
Tx= sleep aide, pain management SE= sedation, priapism, dizziness, hypotension, nausea |
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St John's Wort
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block reuptake NE, 5-HT, DA
CytP450 induction Tx= mild-moderate depression SE= photosensitivity, serotonin syndrome |
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Schizophrenia positive Sx
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Limbic system increased DA activity
Characterized by Sx= abnormality/exaggeration of function, hallucinations, delusions, bizzare behavior |
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Schizophrenia negative Sx
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Prefrontal cortex alteration
Characterized by Sx= loss of function, lack of affect, antisocial |
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DARPP-32 protein
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Protein mediates enkephalin effects in striatum
Regulated by D1^2 Decreased in Schizoprenia |
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DA receptors in Schizophrenia
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D2 modulates antipsychotic potency
D4 modulated by clozapine DA receptor increased |
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Nigrotriatal system
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Control of posture and voluntary movements
Substantia nigra->caudate/putamen Parkinson's (dec) Extrapyramidal symptoms (drugs) |
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Mesolimbic-mesocortical system
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Higher mental functions/emotions
Ventral messencephalon->limbic/neocortex Psychosis (inc) |
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Pituitary projections
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DA inhibits prolactin secretion
Mammotrophic cells |
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Chlorpromazine (Thorazine)
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First Antipsychotic - downer
(-)D2, A-adrenergic, histamine receptors Low potency High (-)ACh Oral^IV Tx= antiemesis, sedation, premature ejaculation, severe itching, mania, drug psychosis SE= Orthostatic hypotension, Neuroleptic Malignant syndrome, hyperprolactemia High (-)adrenergic Low EPS Mild jaundice, seizures |
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Fluphenazine (Premitil)
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Phenothiazine
Antipsychotic Classical drug Selective D2 receptor High potency Low anticholinergic SE= High extrapyramidal Low adrenergic blockade |
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Pimozide (Orap)
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Butyrophenone
Antipsychoticonly D2 receptors Similar to haloperidol Tx= Tourette's motor and phonic tics SE= ECG changes (QT) High extrapyramidal Moderate sedative, anticholinergic |
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Clozapine (Clozaril)
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Dibenzodiazepine
D4^5HT2A, alpha1^histamine receptors Tx= delusions^psychosis w/ Parkinson's, tardive dyskinesia, failure to respond SE= Agranulocytosis, hypersensitivity Low extrapyramidal High adrenergic, |
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Classical Antipsychotic drug effects
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Drug effects=
decrease positive Sx increase negative Sx Tx= Schizophrenia, Autism |
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Classical Antipsychotic SE
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Drug SE=
Extrapyramidal effects Adrenergic blockade effects Tx= anticholinergic |
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Tardive Dyskinesia
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Characterized by SSx=
uncontrollable movements in face, trunk, extremities SE of antipsychotics |
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DA blockade (-) endocrine effects
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Antipsychotic SE=
Suppresses appetite^deregulates temp Weight gain Hyperprolactinemia |
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Neuroleptic Malignant Syndrome
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Syndrome characterized by SSx=
muscle rigidity, fever, autonomic instability and cognitive delirium, (+)CPK Tx= antipyretic, hydration, dantrolene, diazepam, bromocriptine |
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Olanzapine (Zyprexa)
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Partial (-)D2^4, 5-HT - downer
Tx= bipolar disorder, negative symptoms of schizoprenia SE= Hyperglycemia, DM-II Low extrapyramidal High adrenergic blockade |
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Risperidone (Risperdal)
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(-) D2, 5-HT2A, blocks alpha
(+) DA at basal ganglia oral w/ active metabolite Tx= First line Schizophrenia, Alzheimer's SE= Lengthens QT, + prolactin High adrenergic blockade Low extrapyramidal |
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Ziprasidone (Geodon)
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Atypical Antipsychotic
Blocks D2^5-HT2A - DA stabilizer oral^IM Tx= Tourette's syndrome, acute mania, negative psychotic Sx SE= Prolongs QT, sedation, hyperprolactinemia, seizures High (-)adrenergic Low EPS |
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Quetiapine (Seroquel)
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Blocks D4^5-HT2A
well tolerated Tx= 1st line for negative/positive Sx of schizophrenia SE= hyperprolactinemia, seizures High adrenergic blockade Low extrapyramidal |
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Aripiprazole (Abilify)
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Atypical antipsychotic - DA stabalizer
Partial D2^5-HT1A agonist 5-HT2A, alpha1, histamine antagonist CYP34A, CYP2D6 Tx= Psychosis SE= hyperglycemia, DM-II, sedation, seizures, decreases esophageal motility Low EPS High (-)adrenergic |
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Carbamazepine (Tegretol)
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Mood stabalizer
Tx= trigeminal neuralgia, bipolar w/ Li combo SE= Hematologic, sore throat, fever, bruising, Stevens Johnson syndrome (skin hypersensitivity; HLA-B1502), GI upset, CNS toxicity DI= antipsychotics (-)efficacy CI= Pregnancy |
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Prochlorperazine (Compazine)
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Antiemetic
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Lithium (Eskalith)
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Bipolar drug
(-) IP3^DAG 0.6-1.2 mEq/L optimal Competes w/Na at proximal tubule Tx= Manic phases of bipolar SE= Tremor, n/d, HA, (-) thyroid, nephrogenic diabetes insipidus, weight gain, mental disorder, muscle weakness, xerostomia, dysgeusia DI= -Na=+Li, thiazides (use Amiloride)^NSAIDs +Li, (-) mani w/ antidepressants |
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Lithium (Eskalith) overdose
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Overdose SSx=
>2.5mEq/L, profuse n/v/d, mental disorder, hyperreflexia, tremor, clonic-tonic, nystagmus, respiratory, cardiac, renal failure |
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Valproic Acid; Divalproex Sodium (Depakene; Depakote)
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Anticonvulsant
rapid OoA Tx= Seizures, bipolar SE= GI upset, increase liver enzymes, weight gain, drowsiness, changes in hair, (-) platelet aggregation |
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Lamotrigine (Lamictal)
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Anticonvulsant - Glutamate downer
Tx= bipolar, seizures SE= rash, GI, CNS |
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Gabapentin (Neurontin)
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Anticonvulsant
Tx= seizures, bipolar, neurological pain SE= Drowsiness, weight gain, HTN, back pain, CNS |
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Parkinsonian SSx
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Related to loss of DA CNS tracts
Characterized by SSx= stiffness, tremor, slowness w/movement, unbalanced, difficulty walking, depression, dementia, postural deformit, difficulty speaking Causes= tumors, trauma, manganese, CO poisoning, metaclopramide (Reglan) |
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L-Dopa (levo-Dopa; Dopar; Larodopa)
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Dopamine precursor
Passes BBB Metabolised in peripheral Tx= Parkinson's SE= n/v |
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Carbidopa (Sinemet)
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Dopa decarboxylase inhibitor
Tx= increases L-dopa effect in Parkinson's treatment |
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L-dopa (Larodopa)/Carbidopa (Sinemet)
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1st line Parkinson's Tx
Short acting, absorption delayed w/ food SE= n/v, HTN, dyskinesia, choreoathetosis, CNS depression, hallucinations, nightmares DI= MAOI, Pyridoxine (Vit B6) CI= Psychosis, closed-angle glaucoma, cardiac, active peptic ulcer, malignant melanoma |
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On-off phenomenon
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Drug associated SE=
L-dopa/Carbidopa Tx of Parkinson's off=akinesia; on=dyskinesia |
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Drug Holiday
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Associated w/ L-dopa/Carbidopa Tx of Parkinson's
Gradual withdrawal -> aknesia^neuroleptic malignant syndrome SE= aspiration pneumonia, pulmonary embolism |
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Selegiline (Deprenyl; Eldepryl)
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(-)MAO-B - upper
Reduces striatal DA metabolism an H202 formation Tx= early stage parkinson's alone late stage w/ L-dopa/carbidopa SE= insomnia (amphetamine-like metabolites) |
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Bromocriptine (Parlodel); Pergolide (Permax)
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Dopamine agonists
Ergot derivatives Tx= decrease need dose of l-dopa/carbidopa for Parkinson's SE= Erythromelalgia (red, tender, swollen feet) anorexia, n/v, constipation, dyspesia, GER, peptic ulcer bleeding, postural hypotension, cardiac arrhythmias, digital vasospasm, CNS illusions |
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Pramipexole (Mirapex); Ropinirole (Requip)
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Dopamine Agonist - DA upper
(D3-D2) Tx= Initial Tx of Parkinson's (well tolerated) SE= nausea, fatigue, narcolepsy |
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Amantadine (Symmetrel)
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Antiviral
(+) DA release - DA upper Tx= influenza, Parkinson's SE= Livedo reticularis, toxic psychosis, seizures, peripheral edema, restlessness, depression insomnia, halucination |
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Benztropine (Cogentin); Biperden (Akineton); Procyclidine (Kemadrin); Trihexyphenidyl (Artane)
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Anticholinergics = ACh downer
Tx= rigidity, tremor, coordination DI= TCA^antihistamines increase effects |
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Tolcapone (Tasmar); Entacapone (Comtan)
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COMT inhibitor - DA upper
prolongs DoA of DA Tx= Adjunct to L-dopa/Carbidopa Tx for Parkinson's SE= Liver disease, dyskinesia, confusion, nausea |
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Alzheimer SSx=
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Related to loss of ACh CNS tracts
Characterized by SSx= confusion, memory loss, disorientation difficulty in activities of daily living, anxiety, paranoia, wandering, pacing, memory disorder Loss of speech, appetite, bladder^bowel control |
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Tacrine (Cognex); Donepezil (Aricept); Rivastigmine (Exelon); Glalantamine (Reminyl)
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(-)AChesterase - ACh uppers
First-line drugs Tx= Initial to slow progression, improve Sx of Alzheimer's SE= liver toxicity (Tacrine), n/v/d, (+) stomach acid production |
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Memantine (Ebixa; Namenda)
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Non-competative antagonist of (NMDA)
Long lasting Alkaline Kidney tubular secretion Tx= severe Alzheimer's, vascular dementia SE= agitation, urinary incontinence, UTI, insomnia, diarrhea DI= (+) dyskinesia^psychiatric disturbances w/ L-dopa Do not administer w/ amantadine^dextromehtorphan |
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Baclofen (Lioresal)
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GABA-B receptor Agonist
Inhibitory Oral, intrathecal Tx= Spasticity, pain SE= drowsiness, muscle weakness, (-) seizure threshold CNS depression w/ interthecal route |
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Tizanidine (Zanaflex)
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A2 adrenergic agonist
Analogue of clonidine Tx= chronic muscle spasticity w/ cord injury, acute muscle spasms SE= sedation, hypotension, dry mouth, weakness |
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Cyclobenzaprine (Flexeril)
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Anticholinergic
Sedative at brain stem Tx= acute muscle spasms SE= sedation, confusion, visual halucinations |
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Carsoprodol (Soma)
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Central sedative
Drug of Abuse Tx= insomnia w/ pain control SE= hepatic microsomal enzyme DI= meprobamate (+) metabolism |
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Botulinum Toxin (Botox)
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Block ACh release
Presynaptic nerve terminals Tx= local muscle spasms due to stroke, remove wrinkles SE= Toxic at large doses |
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Ziconotide (Prialt)
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Blocks neuronal calcium channels
Venom derivative (snail-Conus magus) Tx= neuropathic pain, acute stroke, protection against brain ischemia, post-op pain, muscle relaxation |
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CNS stimulant SSx
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Inhibit reuptake^promote release of catecholamines
Drug characterized by SSx= (+) BP w/ reflex bradycardia, bronchial relaxation, euphoria, excitement, increased alertness, reduced appetite stimulation of respiration, tremor, CNS stimulation Stereotypic movements, paranoia, CNS illusions, aggression, psychosis |
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Methylphenidate (Ritalin); Dexmethylphenidate (Focalin); Pemoline (Cylert)
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CNS stimulant
DA uptake blockade Tx= narcolepsy, ADHD SE= withdrawal, addictive behaviors, n/v/d, HA, anxiety |
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Modafinil (Provigil)
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Psychostimulant
(+) glutamate transmission Acts in thalamus^hippocampus Induces CYP3A4 Tx= narcolepsy SE= n/v/d, HA, anxiety DI= (+) efficacy w/ (+)A-adrenergic (-) efficacy of contraceptives^cyclosporines (+) organ rejection w/ transplant |
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Dexfenfluramine (Redux)
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Promotes (+)5-HT
Tx= appetitie suppressant, antidepresant SE= pulmonary HTN |
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Phentermine + Fenfluramine (Phen-fen)
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(+)DA^5-HT
Tx= appetite suppresant SE= heart valve abnormalities |
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Antidepressant FDA Black Box warning (BBW)
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Drug BBW
Increased suicide risk in adolescents and children |
