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Pronunciation |
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(meth
am FET a
meen) |
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U.S. Brand
Names |
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Desoxyn® |
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Generic
Available |
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No |
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Synonyms |
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Desoxyephedrine Hydrochloride; Methamphetamine Hydrochloride |
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Pharmacological Index |
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Stimulant |
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Use |
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Treatment of ADHD; exogenous obesity (short-term adjunct)
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Restrictions |
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C-II |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Known hypersensitivity or idiosyncrasy to sympathomimetic amines; patients
with advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to
severe hypertension (stage II or III), hyperthyroidism, glaucoma, agitated
states; patients with a history of drug abuse; use during or within 14 days
following MAO inhibitor therapy; stimulant medications are contraindicated for
use in children with attention deficit/hyperactivity disorders and concomitant
Tourette's syndrome or tics |
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Warnings/Precautions |
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Use with caution in patients with bipolar disorder, diabetes mellitus,
cardiovascular disease, seizure disorders, insomnia, porphyria, or mild
hypertension (stage I). May exacerbate symptoms of behavior and thought disorder
in psychotic patients. Potential for drug dependency exists - avoid abrupt
discontinuation in patients who have received for prolonged periods. Use in
weight reduction programs only when alternative therapy has been ineffective.
Products may contain tartrazine - use with caution in potentially sensitive
individuals. Stimulant use in children has been associated with growth
suppression. |
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Adverse
Reactions |
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Cardiovascular: Hypertension, tachycardia, palpitations
Central nervous system: Restlessness, headache, exacerbation of motor and
phonic tics and Tourette's syndrome, dizziness, psychosis, dysphoria,
overstimulation, euphoria, insomnia
Dermatologic: Rash, urticaria
Endocrine & metabolic: Change in libido
Gastrointestinal: Diarrhea, nausea, vomiting, stomach cramps, constipation,
anorexia, weight loss, xerostomia, unpleasant taste
Genitourinary: Impotence
Neuromuscular & skeletal: Tremor
Miscellaneous: Suppression of growth in children, tolerance and withdrawal
with prolonged use |
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Overdosage/Toxicology |
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Symptoms of overdose include seizures, hyperactivity, coma, hypertension
There is no specific antidote for amphetamine intoxication and the bulk of
the treatment is supportive. Hyperactivity and agitation usually respond to
reduced sensory input, however with extreme agitation haloperidol (2-5 mg I.M.
for adults) may be required. Hyperthermia is best treated with external cooling
measures, or when severe or unresponsive, muscle paralysis with pancuronium may
be needed. Hypertension is usually transient and generally does not require
treatment unless severe. For diastolic blood pressures >110 mm Hg, a
nitroprusside infusion should be initiated. Seizures usually respond to diazepam
IVP and/or phenytoin maintenance regimens. |
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Drug
Interactions |
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CYP2D6 enzyme substrate
Methamphetamine may decrease hypotensive effects of guanethidine
Methamphetamine is contraindicated with MAOIs
Antipsychotics may antagonize the CNS stimulant effect of methamphetamine
Concurrent use of methamphetamine and TCAs and indirect-acting
sympathomimetic amines should be dosed carefully |
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Mechanism of
Action |
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A sympathomimetic amine related to ephedrine and amphetamine with CNS
stimulant activity; peripheral actions include elevation of systolic and
diastolic blood pressure and weak bronchodilator and respiratory stimulant
action |
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Pharmacodynamics/Kinetics |
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Duration: 12-24 hours |
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Usual Dosage |
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Attention deficit disorder: Children >6 years: 2.5-5 mg 1-2 times/day, may
increase by 5 mg increments weekly until optimum response is achieved, usually
20-25 mg/day
Exogenous obesity: Children >12 years and Adults: 5 mg, 30 minutes before
each meal; long-acting formulation: 10-15 mg in morning; treatment duration
should not exceed a few weeks |
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Dietary
Considerations |
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Should be administered 30 minutes before meals |
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Monitoring
Parameters |
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Heart rate, respiratory rate, blood pressure, and CNS
activity |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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Use vasoconstriction with caution in patients taking methamphetamine.
Amphetamines enhance the sympathomimetic response of epinephrine and
norepinephrine leading to potential hypertension and
cardiotoxicity. |
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Dental Health:
Effects on Dental Treatment |
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Up to 10% of patients taking dextroamphetamines may present with
hypertension. The use of local anesthetic without vasoconstrictor is recommended
in these patients. |
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Patient
Information |
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Take exactly as directed (do not increase dose or frequency without
consulting prescriber); may cause physical and/or psychological dependence. Do
not crush extended release tablets. Take early in day to avoid sleep
disturbance, 30 minutes before meals. Avoid alcohol, caffeine, or OTC
medications that act as stimulants. You may experience restlessness, false sense
of euphoria, or impaired judgment (use caution when driving or engaging in tasks
requiring alertness until response to drug is known); dry mouth (frequent small
meals, frequent mouth care, sucking lozenges, or chewing gum may help); nausea
or vomiting (small frequent meals, frequent mouth care may help); constipation
(increased exercise, dietary fiber, fruit, or fluid may help); diarrhea
(buttermilk, boiled milk, or yogurt may help); or altered libido (reversible).
Diabetics need to monitor serum glucose closely (may alter antidiabetic
medication requirements). Report chest pain, palpitations, or irregular
heartbeat; extreme fatigue or depression; CNS changes (aggressiveness,
restlessness, euphoria, sleep disturbances); severe unremitting abdominal
distress or cramping; blackened stool; changes in sexual activity; or blurred
vision. Pregnancy/breast-feeding precautions: Inform prescriber if you
are or intend to be pregnant. Do not breast-feed. |
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Nursing
Implications |
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Dose should not be given in evening or at bedtime; do not crush extended
release tablet |
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Dosage Forms |
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Tablet, as hydrochloride: 5 mg
Tablet, extended release, as hydrochloride (Gradumet®):
5 mg, 10 mg, 15 mg |
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References |
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Catanzarite VA and Stein DA,
"'Crystal' and Pregnancy: Methamphetamine-Associated Maternal Death," West J
Med, 1995, 162(5):454-7.
Gilbert RB, Peng PI,and Wong D,
"A Labetalol Metabolite With Analytical Characteristics Resembling Amphetamines,"
J Anal Toxicol, 1995, 19(2):84-6.
Gospe SM Jr,
"Transient Cortical Blindness in an Infant Exposed to Methamphetamine," Ann
Emerg Med, 1995, 26(3):380-2.
McKinney PF, Tomaszewski C, Phillips S, et al,
"Methamphetamine Toxicity Prevented by Activated Charcoal in a Mouse Model,"
Ann Emerg Med, 1994, 24(2):220-2.
Mendelson J, Jones RT, Upton R, et al,
"Methamphetamine and Ethanol Interactions in Humans," Clin Pharmacol
Ther, 1995, 57(5):559-68.
Mueller PD and Korey WS, "Death by Ecstasy - The Serotonin Syndrome?" Clin
Toxicol, 1995, 33(5):550.
Nestor TA, Tamamoto WI, Kam TH, et al,
"Acute Pulmonary Oedema Caused by Crystalline Methamphetamine," Lancet,
1989, 2(8674):1277-8.
Richards CF, Clark RF, Holbrook T, et al,
"The Effect of Cocaine and Amphetamines on Vital Signs in Trauma Patients," J
Emerg Med, 1995, 13(1):59-63.
Rothrock JF, Rubenstein R, and Lyden PD,
"Ischemic Stroke Associated With Methamphetamine Inhalation," Neurology,
1988, 38(4):589-92.
Segar DL, "Substances of Abuse: Topics," Emerg Med, 1985, 7:18-30.
Sperling LS and Horowitz JL,
"Methamphetamine-Induced Choreoathetosis and Rhabdomyolysis," Ann Intern
Med, 1994, 121(12):986. |
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