TIZANIDINE HYDROCHLORIDE capsule, gelatin coated

Země: Spojené státy

Jazyk: angličtina

Zdroj: NLM (National Library of Medicine)

Aktivní složka:

TIZANIDINE HYDROCHLORIDE (UNII: B53E3NMY5C) (TIZANIDINE - UNII:6AI06C00GW)

Dostupné s:

AvKARE

INN (Mezinárodní Name):

TIZANIDINE HYDROCHLORIDE

Složení:

TIZANIDINE 2 mg

Podání:

ORAL

Druh předpisu:

PRESCRIPTION DRUG

Terapeutické indikace:

Tizanidine is a central alpha-2-adrenergic agonist indicated for the management of spasticity. Because of the short duration of therapeutic effect, treatment with tizanidine should be reserved for those daily activities and times when relief of spasticity is most important [see Dosage and Administration (2.1)]. Tizanidine is contraindicated in patients taking potent inhibitors of CYP1A2, such as fluvoxamine or ciprofloxacin [see Drug Interactions (7.1,7.2)]. Pregnancy Category C Tizanidine has not been studied in pregnant women. Tizanidine should be given to pregnant women only if the benefit outweighs the risk to the unborn fetus. Reproduction studies performed in rats at a dose of 3 mg/kg, equal to the maximum recommended human dose on a mg/m 2 basis, and in rabbits at 30 mg/kg, 16 times the maximum recommended human dose on a mg/m 2 basis, did not show evidence of teratogenicity. Tizanidine at doses that are equal to and up to 8 times the maximum recommended human dose on a mg/m 2 basis increased gestation duration in rats. Prenatal and postnatal pup loss was increased and developmental retardation occurred. Post-implantation loss was increased in rabbits at doses of 1 mg/kg or greater, equal to or greater than 0.5 times the maximum recommended human dose on a mg/m 2 basis. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when tizanidine is administered to a nursing woman. Safety and effectiveness in pediatric patients have not been established. Tizanidine is known to be substantially excreted by the kidney, and the risk of adverse reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function. Clinical studies of tizanidine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently than younger subjects. Cross-study comparison of pharmacokinetic data following single dose administration of 6 mg tizanidine showed that younger subjects cleared the drug four times faster than the elderly subjects. In elderly patients with renal insufficiency (creatinine clearance <25 mL/min), tizanidine clearance is reduced by more than 50% compared to healthy elderly subjects; this would be expected to lead to a longer duration of clinical effect. During titration, the individual doses should be reduced. If higher doses are required, individual doses rather than dosing frequency should be increased. Monitor elderly patients because they may have an increased risk for adverse reactions associated with tizanidine. Tizanidine is known to be substantially excreted by the kidney, and the risk of adverse reactions to this drug may be greater in patients with impaired renal function. In patients with renal insufficiency (creatinine clearance < 25 mL/min) clearance was reduced by more than 50%. In these patients, during titration, the individual doses should be reduced. If higher doses are required, individual doses rather than dosing frequency should be increased. These patients should be monitored closely for the onset or increase in severity of the common adverse events (dry mouth, somnolence, asthenia and dizziness) as indicators of potential overdose [see Dosage and Administration (2.2),Warnings and Precautions (5.7) and Clinical Pharmacology (12.3)]. The influence of hepatic impairment on the pharmacokinetics of tizanidine has not been evaluated. Because tizanidine is extensively metabolized in the liver, hepatic impairment would be expected to have significant effects on pharmacokinetics of tizanidine [see Dosing and Administration (2.3), Warnings and Precautions (5.2), and Clinical Pharmacology (12.3)]. Abuse potential was not evaluated in human studies. Rats were able to distinguish tizanidine from saline in a standard discrimination paradigm, after training, but failed to generalize the effects of morphine, cocaine, diazepam, or phenobarbital to tizanidine. Tizanidine is closely related to clonidine, which is often abused in combination with narcotics and is known to cause symptoms of rebound upon abrupt withdrawal. Three cases of rebound symptoms on sudden withdrawal of tizanidine have been reported. The case reports suggest that these patients were also misusing narcotics. Withdrawal symptoms included hypertension, tachycardia, hypertonia, tremor, and anxiety. Withdrawal symptoms are more likely to occur in cases where high doses are used, especially for prolonged periods, or with concomitant use of narcotics. If therapy needs to be discontinued, the dose should be decreased slowly to minimize the risk of withdrawal symptoms [see Dosage and Administration (2.2)]. Monkeys were shown to self-administer tizanidine in a dose-dependent manner, and abrupt cessation of tizanidine produced transient signs of withdrawal at doses > 35 times the maximum recommended human dose on a mg/m 2 basis. These transient withdrawal signs (increased locomotion, body twitching, and aversive behavior toward the observer) were not reversed by naloxone administration.

Přehled produktů:

Tizanidine Hydrochloride Capsules 2 mg are available as hard gelatin capsules with blue opaque body and blue opaque cap imprinted “APO T2” in black ink. They are supplied as follows: Bottles of 150 NDC 42291-810-15 Tizanidine Hydrochloride Capsules 4 mg are available as hard gelatin capsules with white opaque body and blue green opaque cap imprinted “APO T4” in black ink. They are supplied as follows: Bottles of 150 NDC 42291-811-15 Tizanidine Hydrochloride Capsules 6 mg are available as hard gelatin capsules with blue opaque body and blue opaque cap imprinted “APO T6” in black ink. They are supplied as follows: Bottles of 150 NDC 42291-812-15 Store at 20 º to 25 º C (68 º to 77 º F); excursions permitted to 15 º to 30 º C (59 º to 86 º F) [see USP Controlled Room Temperature]. Dispense in a tight, light-resistant container [see USP]. Dispense in containers with child resistant closure.

Stav Autorizace:

Abbreviated New Drug Application

Charakteristika produktu

TIZANIDINE HYDROCHLORIDE- TIZANIDINE HYDROCHLORIDE CAPSULE, GELATIN
COATED
AVKARE
----------
HIGHLIGHTS OF PRESCRIBING INFORMATION
TIZANIDINE HYDROCHLORIDE CAPSULES
RX ONLY
THESE HIGHLIGHTS DO NOT INCLUDE ALL THE INFORMATION NEEDED TO USE
TIZANIDINE
HYDROCHLORIDE CAPSULES SAFELY AND EFFECTIVELY. SEE FULL PRESCRIBING
INFORMATION FOR
TIZANIDINE HYDROCHLORIDE CAPSULES.
TIZANIDINE HYDROCHLORIDE CAPSULES, FOR ORAL USE
INITIAL U.S. APPROVAL: 1996
INDICATIONS AND USAGE
Tizanidine is a central alpha-2-adrenergic agonist indicated for the
management of spasticity. Because of
the short duration of therapeutic effect, treatment with tizanidine
should be reserved for those daily
activities and times when relief of spasticity is most important. (1)
DOSAGE AND ADMINISTRATION
Recommended starting dose: 2 mg; dose can be repeated at 6 to 8 hour
intervals, up to a maximum of
3 doses in 24 hours (2.1)
Dosage can be increased by 2 mg to 4 mg per dose, with 1 to 4 days
between increases; total daily
dose should not exceed 36 mg (2.1)
Tizanidine pharmacokinetics differs between tablets and capsules, and
when taken with or without food.
These differences could result in a change in tolerability and control
of symptoms (2.1,12.3)
To discontinue tizanidine, decrease dose slowly to minimize the risk
of withdrawal and rebound
hypertension, tachycardia, and hypertonia (2.2)
DOSAGE FORMS AND STRENGTHS
Capsules 2 mg, 4 mg and 6 mg (3)
CONTRAINDICATIONS
Concomitant use with potent inhibitors of CYP1A2, such as fluvoxamine
or ciprofloxacin (4,5.5,7.1,7.2)
WARNINGS AND PRECAUTIONS
Hypotension: monitor for signs and symptoms of hypotension, in
particular in patients receiving
concurrent antihypertensives; tizanidine should not be used with other
α
-adrenergic agonists (5.1,7.7)
Risk of liver injury: monitor ALTs; discontinue tizanidine if liver
injury occurs (5.2)
Sedation: Tizanidine may interfere with everyday activities; sedative
effects of tizanidine, alcohol, and
other CNS depressants are additive (5.3,7.5,7.6)
Hallucinations: consider dis