CNS Drugs Flashcards
Amphetamines
Ritalin
Indicated for: Narcolepsy, weight control, and ADHD
MOA: Stimulates all areas of the brain by increasing the release of norepinephrine and dopamine in the brain. Sympato-mimetic. Responses include increased alertness, wakefulness, decreased fatigue, mood elevation/euphoria, increased initiative, and decreased appetite
May cause: Nervousness, anxiety, sleeplessness, increased HR, increased BP, arrhythmias, sleeplessness and excessive crying and growth suppression in children, and possible bone marrow suppression
Contraindicated for: Insomnia/psychological disorders, hypertension, cardiac arrhythmias, and anorexia.
Drug interactions: Anticholinergics, anticoagulants, anticonvulsants, and tricyclic antidepressants
POTENTIAL FOR ABUSE
Xanthines
Caffeine, Theobromine, Theophylline/Aminophylline
Indicated for: Pain from headache, asthma, bronchitis, emphysema, and drowsiness (Minimal therapeutic usefulness)
MOA: Increases CNS activity by inhibiting breakdown of cyclic AMP. Responses include CNS stimulation, cardiac stimulation, blood vessel constriction in the brain, diuresis, and bronchiorelaxation
May cause: Increased HR, cardiac arrhythmia, increased gastric secretions (esp. caffeine), diuresis, excess CNS stimulation (convulsions, insomnia), and headache and irritability upon withdrawal
Contraindicated for: Cardiac arrhythmia, ulcers, and excessive consumption during pregnancy
ACTIVATE CP450 ENZYMES, POSSIBLE DRUG INTERACTIONS
Cocaine
Lidocaine, Benzocaine
Indicated for: Local anesthetic (ONLY FDA-approved use)
MOA: Stimulates all areas of the brain by increasing the release of norepniephrine and dopamine in the brain. Local effects not understood.
May cause: Initially anxiety, restlessness, confusion, dizziness, tremors, convulsions, then later depression, unconsciousness, bradycardia, hypotension, cardiac arrest, and possible death. Allergic reactions not common, but possible
Contraindicated for: Any use other than as a local anesthetic
Barbiturates
Phenobarbital
Indicated for: Situational and neurotic anxiety, sedation, anti-convulsant, sleep disorders, and general anesthesia
MOA: Possible inhibition of the reticular activating system. GABA independent.
May cause: Drowsiness, impared performance, decreased perception, impaired judgment, hyperalgesia, respiratory depression, and a hangover effect with serious withdrawal symptoms possible when discontinued
Contraindicated for: Taking with other sedative-hypnotics, tendency for drug abuse, and pregnancy.
May be taken orally
Speed and duration of action depend upon different kinds available
ACTIVATE CP450 ENZYMES, POSSIBLE DRUG INTERACTIONS
NO ANALGESIA, CAUSES HYPERALGESIA
Benzodiazepines
Diazepam
Indicated for: Situational and neurotic anxiety, sedation, anti-convulsant, sleep disorders, and general anesthesia
MOA: Binds to a special receptor to decrease brain activity and also increase GABA activity. GABA-dependent.
May cause: Drowsiness, impaired performance, decreased perception, impaired judgment, anterograde amnesia, respiratory depression, and possible hangover effect with severe withdrawal symptoms when discontinued
Contraindicated for: Taking with other sedative-hypnotics, tendency for drug abuse, and pregnancy.
Overdose may be reversed by competitive antagonist flumazenil
ACTIVATE CP450 ENZYMES, POSSIBLE DRUG INTERACTIONS
NO ANALGESIA
Ethyl alcohol
Indicated for: None
MOA: Increase in GABA activity during short-term use. Long-term use sees decrease of depressive effects.
May cause: Drowsiness, impaired performance, decreased perception, impaired judgment, cerebellar atrophy, respiratory depression, and possible hangover effect with severe withdrawal symptoms when discontinued
Contraindicated for: Head trauma, taking with other sedative-hypnotics, tendency for drug abuse, and pregnancy.
ACTIVATE CP450 ENZYMES, POSSIBLE DRUG INTERACTIONS
Goals of Anesthesia
1) Analgesia
2) Amnesia and loss of consciousness
3) Muscle relaxation
Inhalation Anesthetics
Isoflurane, Nitrous Oxide
CNA depressants
Responses: Loss of consciousness, amnesia
May cause: Respiratory depression, lowered blood pressure, decreased heart rate, arrhythmia, malignant hypothermia, and post-operative nausea and vomiting
Nitrous oxide acts as an adjunct only
Thiopental (Barbiturate)
Intravenous anesthetic
Causes loss of consciousness, hyperalgesia
May cause: Respiratory depression, lowered blood pressure, decreased heart rate, malignant hypothermia, and post-operative nausea and vomiting
NO ARRHYTHMIA
IV administration works in seconds, is eliminated quickly
Ketamine
NOT a CNS depressant
NO RESPIRATORY DEPRESSION, NO SKELETAL MUSCLE RELAXATION
May cause: Increased respiration, increased heart rate, analgesia without loss of consciousness at low dose, loss of consciousness at higher dose, and nightmares and hallucinations upon regaining consciousness
Antiepilectic Agents/Anticonvulsant Drugs
Indicated for: Seizures
MOA: Decreased CNS excitability by changing electrolyte movement or changing neurotransmitter (increase GABA, decrease glutamate)
Adverse effects: Sedation, kidney damage, liver damage, blood diseases
Levodopa
Indicated for: Parkinsonism
MOA: Moves more dopamine into the brain, increasing its availability
May cause: Jerking movements, drooling, anorexia, nausea, vomiting, palpitations, arrhythmias, blood pressure changes, orthostatic hypertension, aggravation of narrow-angle glaucoma, and compulsive behavior
Used in combination with carbidopa
Must be discontinued slowly
Anticholinergic drugs
Indicated for: Parkinsonism
MOA: Blocks muscarinic receptors in brain, decreases acetylcholine receptivity of brain
May cause: Confusion, insomnia
Must be discontinued slowly
Carbidopa
Indicated for: Parkinsonism
MOA: Prevents conversion of levodopa to dopamine peripherally, but not centrally
Decreases side effects of levodopa when used in conjuction
Narcotics
Opioids
Indicated for: Pain relief without loss of consciousness, cough suppression (antitussive), and chronic/acute diarrhea
MOA: Blocks mu and kappa receptors in the CNS to decrease the release of substance p and inhibit excitatory transmissions from nerve terminals carrying painful stimuli
May cause: Stimulation of the brain’s emetic center, respiratory depression, constipation, restlessness, excitement, tremors, delirium, insomnia, and physical dependence
Contraindicated for: Respiratory depression/emphysema and head injuries
Withdrawal symptoms: Chills, hot flashes, tearing, runny nose, sneezing, drowsiness, anxiety, twitching, cramps, vomiting, diarrhea, diluted pupils, elevated body temperature, increased heart rate, and increased blood pressure
TENDENCY FOR TOLERANCE, ABUSE, AND PHYSICAL DEPENDENCE
Salicylates
Aspirin
Indicated for: Analgesic (including arthritis), antipyretic, antiinflammatory, and anticoagulant
MOA: COX-2 inhibition
May cause: GI irritation, decreased coagulation, CNS stimulation, respiratory stimulation leading to alkylosis, irreversible hearing loss, dizziness, decrease in GFR, possible link to Reye’s Syndrome when given during infection
Contraindicated for: Bleeding disorders
Aniline-Tyoe Drugs and Aniline Derivatives
Acetaminophen
Indicated for: Analgesic (excluding arthritis), antipyretic
May cause: Kidney or liver damage, anemia, possible link to bladder cancer
Overdose treated with acetylcysteine may prevent hepatic damage
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
Diclofenac, Flurbiprofen, Ibuprofen, Ketorolac, Piroxicam, Naproxen, Diflunisal
Indicated for: Rheumatoid arthritis, antipyretic, pain relief
MOA: Prostaglandin inhibition by inhibition of COX-2
May cause: Kidney and liver damage, may increase instance of heart attack and stroke
NO ANTICOAGUALTION, MINIMAL GI EFFECTS
Steroids
Indicated for: Inflammation (antipyretic)
Many side effects, including suppression of adrenal glands and suppression of ability to respond to stress
Tricyclics
Amitriptyline, Imipramine
Indicated for: Severe depression (situational depression or endogenous depression)
MOA: Inhibits reuptake of norepinephrine in the synapse to increase presence of norepinephrine. Blocks serotonergic, alpha-adrenergic, histamine, and muscarinic receptors
May cause: Sedation, blurred vision, dry mouth, urinary retention, constipation, hypotension, arrhythmias, and sexual dysfunction
Contraindicated for: Hypotension, cardiac arrhythmias, and interactions with other sympatomimetic drugs
Cholinergic rebound symptoms: Nausea, anorexia, insomnia, depression, and anxiety
Monoamine Oxidase Inhibitors
Indicated for: Depression and hyertension
MOA: Increases norepinephrine, then decreases norepinephrine, which is replaced with tyrosine
May cause: CNS stimulation (agitation, restlessness, insomnia), hypotension, hypertensive crisis during food interactions, GI upset, blurred vision, dry mouth, urinary retention in older patients
Contraindicated for: Drug and food interactions, renal failure
Selective Serotonin Reuptake Inhibitors (SSRIs)
Fluoxetine, Escitalopram
Indicated for: Depression
MOA: Inhibits the reuptake of serotonin, prolonging its presence in the synapse. Minimal blocking of muscarinic, alpha-adrenergic, and histamine receptors/
May cause: Nausea, nervousness, headache, insomnia, weight gain, weakness, and sexual dysfunction.
Less orthostatic hypotension and anticholinergic effects than other antidepressants
MAY TAKE UP TO 3 MONTHS TO TAKE EFFECT
Beta Blockers
Indicated for: Temporary stress (NOT FDA APPROVED)
MOA: Stops pounding heart and other immediate stress responses.
EXPERIMENTAL
Buspirone
Indicated for: Anxiety
May cause: Headaches, dizziness, nervousness, nausea, and light-headedness
No euphoria/CNA depression, thus non-addictive
No synergystic effects with alcohol
May take 1 - 2 weeks to take effect
Lithium
Indicated for: Bipolar disorder
MOA: Decreases release of norepinephrine and increases reuptake
May cause: Fatigue, muscle weakness, ataxia, slurred speech, fine tremor of hands, nausea, vomiting, diarrhea, polydipsia, polyuria, polyphagia, renal change, hypothyroidism
Contraindicated for: Abnormal sodium intake and pregnancy
LOW THERAPEUTIC INDEX
COX-2 Inhibitors
Indicated for: Pain management (not available in the U.S.)
MOA: Inhibit COX-2 from producing prostaglandins.
Because COX-2 is not present in GI tissue, side effects do not include GI symptoms.
May cause: Liver damage, kidney damage, and bone marrow damage. Increased instance of cardiac deaths occur than for other NSAIDs.
