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Pharm 20-24
CNS stimulants, CNS depressants, anticonvulsants, Neuromusc
| Question | Answer |
|---|---|
| Central Nervous System | Brain and spinal cord |
| Amphetamines | stimulate the release of neurotransmitters (norepinephrine and dopamine); Adderall controls ADHD; causes euphoria and alertness |
| Amphetamines (side effects and adverse effects) | restlessness, insomnia, tachycardia, HTN, heart palpitations, dry mouth, anorexia, weight loss, diarrhea, constipation, impotence |
| Methylphenidate (prototype; trade name, contraindications; pregnancy category) | amphetamine-like drug (CNS stimulant) Trade Name: Ritalin/Ritalin SR Pregnancy Category: C Contraindications: hypersensitivity, hyper thyroidism, anxiety, history of seizures, motor tics, Tourette syndrome, glaucoma NOT to be used in children under 6 |
| Methylphenidate (prototype; Pharmacokinetics and pharmacodynamics) | Kinetics: Well absorbed from GI Half life: 1-3 hours Excretion: 40% unchanged in urine Dynamics: PO: onset = .5-1 hr; peak = 1-3 hours; duration = 4-6 hr |
| Methylphenidate (prototype; Dosage; Drug-Lab-Food Interactions) | ADHD: PO, 5 mg before breakfast and lunch Narcolepsy: PO, 10 mg, BID/TID before meals Drug interactions: may increase effects of decongestants, antiHTN, barbiturates; alter insulin Food: caffeine may increase effects |
| Methylphenidate (prototype; uses) | correct hyperactivity caused by ADHD, increase attention span, treat fatigue, and control narcolepsy |
| Anorexiants (definition, use, side effects) | appetite suppressants; treat obesity; rarely prescribed; Didrex, Dexedrine, Dospan; do NOT give to children younger than 12 y.o.; nervousness, restlessness, irritability, insomnia, heart palpitations, HTN |
| Analeptics (definition, use, side effects) | CNS stimulant; stimulate respiration; may contain caffeine; used to stimulate increased respirations in newborns; nervousness, restlessness, tremors, twitching, palpitations, insomnia, diuresis, GI irritation, tinnitus; t1/2 = 3.5 hours |
| Doxapram (Dopram) | CNS and respiratory stimulant used to treat respiratory depression caused by drug OD, pre- and postanesthetic resp depression, COPD; IV c onset of 20-40 minutes and peaks at 2 minutes; HTN, tachycardia, trembling, and convulsions |
| Migraine headaches | characterized by a unilateral throbbing HEAD pain c nausea, vomiting, photophobia; caused by inflammation and dilation of blood vessels in cranium; etiology unknown; classic = aura, common = no aura |
| Cluster headaches | characterized by a severe unilateral NONthrobbing pain located around EYE; NO aura, NO nausea, NO vomiting |
| Migraine treatment | analgesics, opioid analgesics, ergot alkaloids, selective serotonin (5-HT) receptor agonists; MILD - aspirin, acetaminophen or NSAIDs; Demerol or Stadol NS |
| Sumatriptan (prototype; drug class, contraindications, dosage) | 5-HT receptor agonist (antimigraine) Trade: Imitrex Pregnancy Category: C Contraindications: hypersenstivity, coronary artery disease, HTN, obesity, diabetes mel., smoking Dosage: SubQ, PO, intranasal |
| REM rebound | results in vivid dreams and nightmares; frequently occurs after taking a hypnotic for a prolonged period then abruptly stopping; it MAY occur after one hypnotic dosage |
| Barbiturates (definition, long, intermediate) | sedative-hypnotic; long-acting = control of seizures in epilepsy (Phenobarbital and mephobarbital) intermediate-acting = sleep sustainers for maintaining sleep (butabarbital AKA Butisol) - ASSESS VITALS |
| Barbiturates (short and ultrashort) | short-acting = induce sleep (secobarbital AKA Seconal, pentobarbital AKA Nembutal - ASSESS VITALS ultrashort-acting = general anesthetic; thiopental sodium AKA Pentothal |
| Secobarbital sodium (prototype; drug class, contraindications, dose) | sedative-hypnotic: barbiturate Trade: Seconal Sodium Pregnancy Category: D Contraindications: resp depression, severe hepatic disease, pregnancy, nephrosis, hypersensitivity Dosage: Sed - PO, Hyp - PO at bedtime, preop - PO 1-2 hr before |
| Secobarbital sodium (prototype; Drug interactions, Pharmacokinetics/dynamics) | Drug interactions: decrease resp c alcohol, CNS depressants, MAOIs Pharmacokinetics: PO - 90% from GI; t1/2 = 15-40 hr; urine excretion as metabolites Pharmacodynamics: PO - onset = 15-30 min; Peak = .5-1 hr; duration = 3-4 hrs |
| Secobarbital sodium (prototype; use, side effects) | treats insomnia; used for sedation, preop medication Side effects: lethargy, drowsiness, hangover, dizziness, paradoxical excitement in elderly |
| Sumatriptan (prototype; pharmacokinetics/dynamics, use) | Pharmacokinetics: rapid absorp following subQ; 10-20% protein bound; t1/2 = 2 hrs; excretion in urine and feces Pharmacodynamics: onset quicker with subQ than PO peak 2-4 hrs c both; duration unknown treat migraine and cluster headaches |
| Sumatriptan (prototype; side effects) | dizziness, fainting, tingling, numbness, warm sensation, drowsiness, muscle cramps, nausea, vomiting, diarrhea, abdom cramping Adverse reactions: hypotension, HTN, heart block, angina, dysrhythmias, thromboembolism, seizures, CNS hemorrhage, stroke |
| Benzodiazepines (Xanax, Ativan, Restoril) | minor tranquilizer, antianxiety agent increase the action of the inhibitory neurotransmitter gamma-amniobutyric acid (GABA) to the GABA receptors; neuron excitability is reduced can suppress stage 4 of REM, not to be used longer than 3-4 wks |
| Nonbenzodiazepines | used for short-term treatment (less than 10 days) for insomnia |
| flumazenil (Romazicon) | benzodiazepine antagonist; reversal of sedative effects; management of benzo OD |
| Zolpidem tartrate (prototype; drug class, contraindications, dosage, interactions) | Sedative-hypnotic; non-benzodiazepine Trade: Ambien Pregnancy Category: B Contraind: allergy, lactation Dosage: PO - at bedtime Interactions: drug - decrease CNS function with alcohol, CNS depress, anticonvuls, phenothiazines; food - decreases absorp |
| Zolpidem tartrate (prototype; pharmacokinetics/dynamics, uses) | pharmacokinetics: PO, 79-96% protein bound; t1/2 = 2-2.5 hrs; excreted in bile, urine, feces pharmacodynamics: PO; onset = 7-27 min; peak = .5-2.3 hrs; duration = 6-8 hrs uses: treat insomnia |
| Zolpidem tartrate (prototype; side effects and adverse reactions) | side effects: drowsiness, lethargy, hangover (residual sedation), irritability, dizziness, anxiety, nausea, vomiting, hypervitaminosis A, bulging fontanelles Adverse: tolerance, psychologic or physical dependence |
| Methylphenidate (prototype; mode of action) | acts primarily on the reticular activating system and cerebral cortex |
| Sumatriptan (prototype; mode of action) | causes vasoconstriction of cranial carotid arteries to relieve migraine attacks |
| Secobarbital sodium (prototype; mode of action) | depression of the CNS, including the motor and sensory activities |
| Zolpidem tartrate (prototype; mode of action) | depression of CNS, neurotransmitter inhibition |
| Anesthetics (general) | depress CNS, alleviate pain, and cause LOC 4 stages: analgesia, excitement/delirium, surgical, medullary paralysis (ventilation NEEDED) IV MED |
| Balanced anesthesia | a hypnotic given the night before, premed c narcotic analgeic or benzodiazepine + anticholinergic, short acting barb, inhaled gas, muscle relaxant * minimizes CV problems, decreases amount of gen anesth. needed, decreases pain; QUICKER RECOVERY |
| Anesthetics (local) | block pain at the site where drug is administered; allows consciousness to be maintained Ethers or amides(low allergy incid) Synthetic cocaine = Novocain Short - .5-1 hr duration Mod - 1-3 hr Long - 3-10 hr |
| Spinal anesthesia | requires local to be injected in the subarachnoid space at the 3rd or 4th lumbar space headaches may result - leaking hypotension - leaking |
| Blocks (nerve, spinal, epidural, caudal, saddle) | Nerve: prevents pain at nerve ending Spinal: subarachnoid membrane (2nd layer) Epidural: outer covering (dura mater) Caudal: near sacrum Saddle: lower end to block perineal area (childbirth) |
| Brain anoxia | lack of oxygen to brain |
| Grand mal (tonic-clonic) seizure | most common; tonic - skeletal muscles contract in a spasm lasting 3-5 seconds; clonic - dysrhythmic muscular contraction, or jerkiness of legs and arms lasting 2-4 minutes; GENERALIZED |
| Petit mal (absence) seizure | brief LOC lasting less than 10 sec; usually occurs in children; fewer than 3 spike waves on EEG; GENERALIZED |
| Psychomotor seizure | complex symptoms - automatisms (repetitive behaviors), behavioral changes, motor seizures; PARTIAL - COMPLEX |
| Motor seizure | Jacksonian Seizure; involves spontaneous movement that spreads, can develop into generalized seizure; PARTIAL - SIMPLE |
| Anticonvulsants | used for epileptic seizures; AKA Antiepileptic drugs (AEDs); suppress the abnormal electric impulses from the seizure focus to other cortical areas - prevents seizure but does not eliminate cause; CNS depressant |
| Phenytoin (prototype; drug class, contraindications, dose) | anticonvulsant, hydantoin Trade: Dilantin Preg Category: D Contraindications: allergy, heart block, psychiatric disorders, pregnancy Dosage: PO and IV (loading dose) Theraputic range: 10-20 mcg/ml Toxic: 30-50 mcg/ml |
| Phentoin (prototype; pharmacokinetics/dynamincs) | pharmacokinetics: PO - slow; IM - erratic; 85-95% protein bound; t1/2 = 6-45 hrs (22); excreted in urine (small), bile/feces (mod) Pharmacodyamics: PO - onset = .5-2 hr, peak = 1.5-3 hr, duration = 6-12 hr; IM - onset = 1 min-1 hr |
| Phentoin (prototype; interactions) | Drug: decreased with folic acid, calcium, antacids Decreases effects of: anticoag, oral contra, antihist, corticoster, dopamine Food: decreased adsorption |
| Phentoin (prototype; uses; side effects and adverse effects) | prevent tonic-clonic (grand mal) and complex partial seizures (psychomotor) Side fx: headache, diplopia, confus, dizzi, sluggishness, decreased coord, slurred spch, rash, anorexia, naus, vomit, red-brwn colored urine Adverse: depress, gingival hyrplasia |
| Phentoin (prototype; mode of action) | reduces motor cortex activity by altering transport of ions |
| Status epilepticus | rapid succession of epileptic seizures; treated c phenobarbital, a long-acting barbiturate |
| Succinimides | used to treat absence or petit mal seizures; acts by decreasing calcium influx thru the t-type Ca channels Ethosuximide (Zarontin) |
| Oxazolidones/Oxazolidinedione | treat petit mal seizures; Trimethadione was first drug developed; many severe side effects |
| Divalproex sodium (Depakote) | treatment of manic episodes in bipolar disorders |
| Benzodiazepines (as an anticonvulsant) | Klonopin, Valium, Ativan |
| Anticholinergics | reduce rigidity in Parkinsonism; inhibit the release of acetylcholine; contraindicated if pt has glaucoma DRY YOU UP |
| Carbidopa-levodopa (prototype; drug class, contraindications, dosage) | antiparkinson: dopaminergic Trade: Sinemet Pregnancy Category: C Contraindications: narrow-angle glaucoma, severe cardiac, renal or hepatic disease Dosage: PO - ratio of 10 carb/100 levo; extended release - 5 carb/200 levo |
| Carbidopa-levodopa (prototype; interactions, use) | Drug: increase HTN crisis c MAOIs; decrease levodopa effect c anticholinergics Lab: may increase BUN, AST, ALT, ALP, LDH Food: avoid foods c vitamin B6 Use: treat parksinsonism; relieve tremors and rigidity |
| Carbodopa-levodopa (prototype; pharmacokinetics/dynamics) | Pharmacokinetics: PO - well absorbed; carbidopa 36% protein bound, levodopa is unknown; t1/2 = 1-2 hrs; excreted in urine as metabolites Pharmacodynamics: PO - onset = 15 min; peak = 1-3 hrs; duration = 5-12 hrs |
| Carbodopa-levodopa (prototype; side effects, adverse effects) | Side effects: anorexia, naus, vomit, dysphagia, fatigue, dizzi, headache, dry mouth, bitter taste, twitching, blurred vision, insomnia Adverse effects: involuntary movements, palpitations, ortho hypotension, urinary rtn, psychosis, severe depres, halluc |
| Carbidopa-levodopa (prototype; mode of action) | transmission of levodopa to brain cells for conversion to dopamine; carbidopa blocks the conversion of levodopa to dopamine in the peripheral nervous system |
| Dopamine agonists | stimulate the dopamine receptors ex: Amantadine (high tolerance); can be used for drug induced parkinsonism |
| MAO-B inhibitor (-ILINE) | the enzyme monoamine oxidase-B (MAO-B) causes catabolism of dopamine; selegILINE inhibits MAO-B - prolongs action of levodopa ex: RasagILINE (Azilect) |
| COMT inhibitors (-CAPONE) | enzyme catechol-O-methyltransferase (COMT) inactivates dopamine; when taken c levodopa - increase amount of levodopa concentration in the brain |
| Acetylcholinesterase inhibitors (AChE) | tacrine (Cognex); donepezil (Aricept); rivastigmine (Exelon); permits more acetylcholine in the neuron receptors; used for Alzheimer's disease |
| Tacrine (prototype; drug class, contraindications, dosage, interactions) | acetylcholinesterase inhibitor Trade: Cognex Contra: liver/renal diseases Dosage: PO qid Interactions: increse ALT, AST |
| Tacrine (prototype; pharmacokinectics/dynamics, use) | Pharmacokinetics: PO - food decreases absorb rate; 50% pro bnd; t1/2 = 3 hrs; excreted in urine Pharmacodynamics: onset = .5 hr; peak = 2 hrs; duration = 24-36 hrs Use: improves memory loss |
| Tacrine (prototype; side effects, mode of action) | Side effects: anorexia, nausea, vomit, diarrhea, dizzi, hdache, constip, rhinitis, depression Mode of action: elevates acetylcholine concentration |
| Myasthenia gravis (MG) | lack of nerve impulses and muscle responses at the myoneural junction Causes: fatigue and muscular weakness of the resp system, facial muscles and extremities Etiology: inadequate secretion of ACh or loss of ACh |
| Multiple sclerosis (MS) | attacks myelin sheath of nerve fiberws, causing lesions (plaques) |
| Myasthenic crisis | severe generalized muscle weakness and may involve the muscles of respiration; stress or inadequate dosing of AChE inhibitors can trigger |
| Cholinergic crisis | overdoing AChE inhibitors Symptoms: miosis (pupil constriction; abnormal), pallor, sweating, vertigo, excess salivation, naus, vomit, ab crmping,diarrhea, bradycardia, involun muscle twitching |
| AChE inhibitors for MG | neostigmate (Prostigmin): short-acting; t1/2 = .5-1 hr; PO q2-4hr pyridostigmine bromide (Mestinon): intermed action; PO q3-6 hrs ambenonium chloride (Mytelase): long-acting; only given if above don't work |
| Pyridostigmine bromide (prototype; drug class, contraindications, interactions) | cholinesterase inhibitor Trade: Mestinon Preg Category: C Contra: GI and GU obstruction, severe renal disease Interactions: decreased effect c atropine, muscle relaxants, antidysrhythmics, magnesium |
| Pyridostigmine bromide (prototype; dosage, use, mode of action) | PO, sustained-release PO, IM/IV, adults and children Use: control and treat myasthenia gravis Mode of action: transmission of neuromuscular impulses by preventing destruction of acetylcholine |
| Pyridostigmine bromide (prototype; pharmacokinetics/dynamics) | Pharmacokinetics: PO - poorly absorbed, Sustained-release - 50%; t1/2 = PO - 3.5-4 hrs, IV - 2 hrs; excreted in urine by liver Pharmacodynamics: IV, IM, PO, PO - SR (quickest to slowest onset); PO SR has longest duration; all peaks are unknown |
| Pyridostigmine bromide (prototype; side effects and adverse reactions) | Side effects: naus, vomit, diarrhea, hdache, dizzi, ab cramps, excess saliva, sweating, rash, miosis Adverse effects: hypotension, bradycardia, urticaria |
| Clients c MS should avoid.... | histamine blockers, idomethacin (an NSAID) and beta-blockers |
| Carisoprodol (prototype; drug class, contraindications, dosage, interactions) | Centrally acting muscle relaxants Trade: Soma, Sopropol Pregnancy category: C Contraindications: severe liver or renal disease Dosage: PO bedtime Interactions: increase CNS depression c alcohol, narcotics, sedative-hypnotics, antihistamines, antidepr |
| Carisoprodol (prototype; pharmacokinetics/dynamics) | Pharmacokinetics: PO - absorbs well; t1/2 = 8 hrs; excreted in urine Pharmacodynamics: PO, onset = 30 mins, Peak = 3-4 hrs, duration = 4-6 hrs |
| Carisoprodol (prototype; mode of action; side effects; adverse effects) | Mode of action: blocks interneuronal activity Side effects: naus, vomit, dizziness, weakness, insomnia Adverse reactions: asthmatic attack, tachycardia, hypotension, diplopia |
Created by:
jodybreeze2013
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