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Comfort Pac w/Tizanidine and Microgestin Fe 1/20

Determining the interaction of Comfort Pac w/Tizanidine and Microgestin Fe 1/20 and the possibility of their joint administration.

Check result:
Comfort Pac w/Tizanidine <> Microgestin Fe 1/20
Relevance: 12.05.2022 Reviewer: Shkutko P.M., M.D., in

In the database of official manuals used in the service creation an interaction registered by statistical results of studies was found, which can either lead to negative consequences for the patient health or strengthen a mutual positive effect. A doctor should be consulted to address the issue of joint drug administration.

Consumer:

Ask your doctor before using ethinyl estradiol together with tiZANidine. This can cause drowsiness, confusion, slow heart rate, shallow breathing, feeling light-headed, fainting, or coma. You may need a dose adjustment if you take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

Professional:

GENERALLY AVOID: Coadministration with oral contraceptives may significantly increase the plasma concentrations and pharmacologic effects of tizanidine. The proposed mechanism is inhibition of tizanidine metabolism via CYP450 1A2. Retrospective evaluation of population pharmacokinetic data following single- and multiple-dose administration of tizanidine revealed an approximately 50% decrease in the clearance of tizanidine in women receiving oral contraceptives compared to women not receiving oral contraceptives. In a study of 30 healthy volunteers administered a single 4 mg dose of tizanidine, mean peak plasma concentration (Cmax) of tizanidine was 3.0 times higher and mean area under the plasma concentration-time curve (AUC) was 3.9 times greater in women using an oral contraceptive containing ethinyl estradiol and gestodene than in women not on the contraceptive. In one contraceptive user, the tizanidine AUC exceeded the mean AUC of the control subjects by nearly 20 times. There were no significant differences in the elimination half-life or time to peak concentration in plasma (Tmax) of tizanidine between the groups. Tizanidine to metabolite ratios in plasma and urine were 2 to 10 times higher in the contraceptive users than in control subjects, and the excretion of unchanged tizanidine into urine was on average 3.8 times greater in the contraceptive group. In addition, both the systolic and diastolic blood pressures were lowered by tizanidine more in the contraceptive users (29 mmHg and 21 mm Hg, respectively) than in the control subjects (17 mmHg and 13 mmHg, respectively). The interaction has also been reported with other CYP450 1A2 inhibitors such as fluvoxamine, ciprofloxacin, and rofecoxib.

MANAGEMENT: The use of tizanidine in combination with oral contraceptives or other CYP450 1A2 inhibitors should generally be avoided. Caution is advised if concurrent use is clinically necessary. Dosage adjustments may be required in patients who experience excessive adverse effects of tizanidine such as drowsiness, dizziness, lightheadedness, hypotension, bradycardia, or syncope.

References
  • Granfors MT, Backman JT, Neuvonen M, Neuvonen PJ "Ciprofloxacin greatly increases concentrations and hypotensive effect of tizanidine by inhibiting its cytochrome P450 1A2-mediated presystemic metabolism." Clin Pharmacol Ther 76 (2004): 598-606
  • Granfors MT, Backman JT, Laitila J, Neuvonen PJ "Oral contraceptives containing ethinyl estradiol and gestodene markedly increase plasma concentrations and effects of tizanidine by inhibiting cytochrome P450 1A2." Clin Pharmacol Ther 78 (2005): 400-11
  • "Product Information. Vioxx (rofecoxib)." Merck & Co, Inc, West Point, PA.
  • "Product Information. Zanaflex (tizanidine)." Acorda Therapeutics, Hawthorne, NY.
  • Momo K, Doki K, Hosono H, Homma M, Kohda Y "Drug interaction of tizanidine and fluvoxamine." Clin Pharmacol Ther 76 (2004): 509-10
  • Granfors MT, Backman JT, Neuvonen M, Ahonen J, Neuvonen PJ "Fluvoxamine drastically increases concentrations and effects of tizanidine: A potentially hazardous interaction." Clin Pharmacol Ther 75 (2004): 331-41
  • Granfors MT, Backman JT, Laitila J, Neuvonen PJ "Tizanidine is mainly metabolized by cytochrome P450 1A2 in vitro." Br J Clin Pharmacol 57 (2004): 349-53
Comfort Pac w/Tizanidine

Generic Name: tizanidine

Brand name: Zanaflex

Synonyms: Tizanidine, TiZANidine

Microgestin Fe 1/20

Generic Name: ethinyl estradiol / norethindrone

Brand name: Blisovi 24 Fe, Blisovi Fe 15/30, Blisovi Fe 1/20, Estrostep Fe, Gildess 24 Fe, Gildess Fe 15/30, Gildess Fe 1/20, Junel Fe 15/30, Junel Fe 1/20, Junel Fe 24, Larin 24 Fe, Larin Fe 15/30, Larin Fe 1/20, Lo Loestrin Fe, Loestrin 24 Fe, Loestrin Fe 15/30, Loestrin Fe 1/20, Lomedia 24 Fe, Microgestin 24 Fe, Microgestin Fe 15/30, Microgestin Fe 1/20, Tarina Fe 1/20, Taytulla, Tilia Fe, Tri-Legest Fe, Blisovi 24 Fe, Femcon Fe, Kaitlib FE, Lo Minastrin Fe, Microgestin 24 Fe, Norinyl 1+35, Ortho-Novum 7/7/7, Tri-Norinyl, Zenchent, femhrt 05 mg/25 mcg, Fyavolv, Jevantique Lo, Jinteli, Femcon Fe, Generess FE, Loestrin 1/20, Ovcon 35, Brevicon

Synonyms: n.a.

In the course of checking the drug compatibility and interactions, data from the following reference sources was used: Drugs.com, Rxlist.com, Webmd.com, Medscape.com.

Interaction with food and lifestyle