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154 Cards in this Set
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Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
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Neuromuscular blocking drugs
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These drugs strongly potentiate and prolong effect of
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Inhaled anesthetics, especially isoflurane,
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neuromuscular blockade (NMB)
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aminoglycosides, and antiarrhythmic
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These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
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Nondepolarizing type antagonists
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Agent with long duration of action and is most likely to cause histamine release
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Tubocurarine
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Non-depolarizing skeletal muscle antagonist that has short duration
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Mivacurium
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Skeletal muscle agent that can block muscarinic receptors
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Pancuronium
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Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
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Atracurium
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One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
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Succinylcholine
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During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
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Cholinesterase inhibitors
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Spasmolytic drugs
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Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
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Spasmolytic drugs
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Facilitates GABA presynaptic inhibition
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Diazepam
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GABA agonist in the spinal cord
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Baclofen
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Similar to clonidine and may cause hypotension
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Tizanidine
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DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
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Dantrolene
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Agent used for acute muscle spasm
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Cyclobenzaprine
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Drugs Used in Parkinsonism & Other Movement Disorders
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Irreversible condition resulting from the use of antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
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Drug induced Parkinsonism
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Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
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L-dopa
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This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
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Carbidopa
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Clinical response that may fluctuate in tx of Parkinson's dx
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"On-off-phenomenon"
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Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
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Levodopa
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Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
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Bromocriptine
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Non ergot agents used as first-line therapy in the initial management of Parkinson's
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Pramipexole and ropinirole
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Enhances dopaminergic neurotransmission SE's include CNS excitation, acute toxic psychosis and livedo reticularis
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Amantadine
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Inhibitor of MAO type B which slows down metabolism of dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
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Selegiline
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Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
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Tolcapone
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Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
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Benztropine
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Agent effective in physiologic and essential tremor
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Propranolol
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Agents used in Huntington's Disease
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Tetrabenazine (amine depleting drug), reserpine
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Agents used in Tourette's dx
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Haloperidol, pimozide , clonidine
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Chelating agent used in Wilson's disease
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Penicillamine
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Antipsychotics
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Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
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Older antipsychotic agents, D2 receptors
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MOA of neuroleptics
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Dopamine blockade
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Side effects occuring in antipsychotics that block dopamine
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Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
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Antipsychotics that reduce positive symptoms only
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Older antipsychotics
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Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
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Olanzapine, aripiprazole, and sertindole
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Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
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Risperidone
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Atypical antipsychotic causing high prolactin levels
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Risperidone
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Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
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Olanzapine
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Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
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Haloperidol
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Drug used in neuroleptic malignant syndrome
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Dantrolene
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Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
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Muscarinic blockers
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Antipsychotic having the strongest autonomic effects
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Thioridazine
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Antipsychotic having the weakest autonomic effects
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Haloperidol
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Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
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Thioridazine
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Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
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Clozapine
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Anti-psychotic not shown to cause tardive dyskinesia
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Clozapine
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Anti-psychotics available in depot preparation
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Fluphenazine and haloperidol
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Reduced seizure threshold
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Low-potency typical antipsychotics and clozapine
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Orthostatic hypotension and QT prolongation
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Low potency phenothiazines and ziprasidone
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Increased risk of developing cataracts
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Quetiapine
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Lithium
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Major route of elimination for Lithium
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Kidneys
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Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
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Lithium toxicity
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Drug increases the renal clearance hence decreases levels of lithium
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Theophylline
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Lithium is associated with this congenital defect
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Cardiac anomalies and is contraindicated in pregnancy or lactation
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DOC for bipolar affective disorder
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Lithium
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Concern using lithium
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Low therapeutic index
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SE of lithium
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Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
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Antidepressants
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Example of three antidepressants that are indicated for obsessive compulsive disorder
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Clomipramine, fluoxetine and fluvoxamine
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Neurotransmitters affected by the action of antidepressants
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Norepinephrine and serotonin
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Usual time needed for full effect of antidepressant therapy
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2 to 6 weeks
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Population group especially sensitive to side effects of antidepressants
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Elderly patients
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All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
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Side-effect profile, drug interaction potential and prior pt response
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Well-tolerated and are first-line antidepressants Monoamine oxidase inhibitors (MAOI)
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SSRI's, bupropion, and venlafaxine
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Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
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Monamine oxidase inhibitors
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Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
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Hypertensive crisis
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MAOI should not be administered with SSRI's or potent TCA's due to development of this condition Tricyclic antidepressants (TCA)
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Serotonin syndrome
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Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
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Tricyclic antidepressants (TCA)
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Three C's associated with TCA toxicity
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Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
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Agents having higher sedation and antimuscarinic effects than other TCA's
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Tertiary amines
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TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
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Amitriptyline
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TCA used in chronic pain, enuresis, and ADD
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Imipramine
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TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
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Doxepin
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TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
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Clomipramine
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Secondary amines that have less sedation and more excitation effect
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Nortriptyline, Desipramine
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Side effects seen with tricyclic antidepressants
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Muscarinic blockade (dry mouth, constipation); weak alpha-1 block (orthostatic hypotension); weak hisamine block (sedation)
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Heterocyclics
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Antidepressant associated with neuroleptic malignant syndrome
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Amoxapine
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Antidepressant associated with seizures and cardiotoxicity
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Maprotiline
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Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
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Venlafaxine
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Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
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Venlafaxine, duloxetine
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Antidepressant also used for sleep that causes priapism
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Trazodone
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Antidepressant which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
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Nefazodone
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Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
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Bupropion
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Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
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Mirtazapine
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SE of mirtazapine
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Liver toxicity, increased serum cholesterol
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Selective serotonin reuptake inhibitors (SSRI)
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Except for these agents all SSRI have significant inhibition of CytP450 enzymes
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Citalopram and its metabolite escitalopram
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Side effects frequently seen with SSRIs
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CNS stimulation; GI upset
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Antidepressants with no effect on BP, no sedation
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SSRIs
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SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
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Fluoxetine
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SSRI indicated for premenstrual dysphoric disorder
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Fluoxetine (Sarafem)
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Some of SSRIs' therapeutic effects beside depression
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Panic attacks, social phobias, bulimia nervosa, and PMDD (premenstrual dysphoric disorder), OCD
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SSRI less likely to cause a withdrawal syndrome
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Fluoxetine
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Opioid Analgesics & Antagonists
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Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
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Ascending pathways
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Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
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Presynaptic mu, delta, and kappa receptors
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Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
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Postsynaptic Mu receptors
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Tolerance to all effects of opioid agonists can develop except
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Miosis and constipation
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All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
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Meperidine
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SE of these drugs include dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
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Opioid Analgesics
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Strong opioid agonists
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Morphine, methadone, meperidine, and fentanyl
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Opioids used in anesthesia
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Morphine and fentanyl
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Opioid used in the management of withdrawal states
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Methadone
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Opioid available trans-dermally
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Fentanyl
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Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
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Morphine
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Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
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Meperidine
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Moderate opioid agonists
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Codeine, hydrocodone, and oxycodone
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Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
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Propoxyphene
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Partial agonist or mixed antagonists
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Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
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Buprenorphine
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Opioid antagonist that is given IV and had short DOA
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Naloxone
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Opioid antagonist that is given orally in alcohol dependency programs
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Naltrexone
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These agents are used as antitussive
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Dextromethorphan, Codeine
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These agents are used as antidiarrheal
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Diphenoxylate, Loperamide
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Drugs of Abuse
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Inhalant anesthetics
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NO, chloroform, and diethyl ether
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Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
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Fluorocarbons and Industrial solvents
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Cause dizziness, tachycardia, hypotension, and flushing
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Organic nitrites
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Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
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Steroids
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Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
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Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
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Opioid Analgesics
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Most commonly abused in health care professionals
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Heroin, morphine, oxycodone, meperidine and fentanyl
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This route is associated with rapid tolerance and psychologic dependence
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IV administration
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Leads to respiratory depression progressing to coma and death
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Overdose of opioids
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Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
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Abstinence syndrome
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Treatment for opioid addiction
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Methadone, followed by slow dose reduction
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This agent may cause more severe, rapid and intense symptoms to a recovering addict
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Naloxone
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Sedative-Hypnotics
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Sedative-Hypnotics action
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Reduce inhibition, suppress anxiety, and produce relaxation
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Additive effects when Sedative-Hypnotics used in combination with these agents
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CNS depressants
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Common mechanism by which overdose result in death
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Depression of medullary and cardiovascular centers
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"Date rape drug"
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Flunitrazepam (rohypnol)
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The most important sign of withdrawal syndrome
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Excessive CNS stimulation (seizures)
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Treatment of withdrawal syndrome involves
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Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
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These agents are CNS depressants
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Ethanol, Barbiturates, and Benzodiazepines
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Stimulants
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Withdrawal from this drug causes lethargy, irritability, and headache
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Caffeine
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W/D from this drug causes anxiety and mental discomfort
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Nicotine
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Treatments available for nicotine addiction
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Patches, gum, nasal spray, psychotherapy, and bupropion
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Chronic high dose abuse of nicotine leads to
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Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
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Tolerance is marked and abstinence syndrome occurs
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Amphetamines
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Amphetamine agents
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Dextroamphetamines and methamphetamine
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These agents are congeners of Amphetamine
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DOM, STP, MDA, and MDMA "ecstasy"
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Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
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Cocaine "super-speed"
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Hallucinogens
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Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of both horizontal and vertical nystagmus is pathognomonic
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PCP
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Removal of PCP may be aided
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Urinary acidification and activated charcoal or continual nasogastric suction
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THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
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Marijuana
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