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Pharm 20-24

CNS stimulants, CNS depressants, anticonvulsants, Neuromusc

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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