Dosing & Uses
Dosage Forms & Strengths
Clostridium Difficile Colitis
Macrolide antibiotic indicated for Clostridium difficile-associated diarrhea in adults
200 mg PO q12hr for 10 days
May take with or without food
Dose adjustment not necessary
Not studied; dose adjustment not necessary since minimally absorbed
<18 years: Safety and efficacy not established
Clostridium difficile Infection (Orphan)
Indicated for Clostridium difficile infection in pediatric patients 16 yr or younger
Orphan indication sponsor
- Optimer Pharmaceuticals, Inc; 10110 Sorrento Valley Road; San Diego, CA 92121
Abdominal pain (6%)
Gastrointestinal hemorrhage (4%)
Increased alkaline phosphatase
Decreased blood bicarbonate
Increased hepatic enzymes
Not indicated for systemic infections
Only use for infection proven or strongly suspected to be caused by C difficile to avoid development of drug resistant bacteria
Acute hypersensitivity reactions, including dyspnea, rash, pruritus, and angioedema of the mouth, throat, and face reported; discontinue and treat appropriately if reaction occurs therapy should be instituted
Some patients with hypersensitivity reactions also reported a history of allergy to other macrolides
Pregnancy & Lactation
Pregnancy Category: B
Lactation: Unknown whether distributed in breast milk; caution advised
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Macrolide antibiotic; bactericidal against C difficile in vitro, inhibiting RNA synthesis by RNA polymerases
Bioavailability: Minimal systemic absorption
Peak Plasma Time: 2 hr (range 1-5 hr)
Peak Plasma Concentration: 5.2 ng/mL (+/- 2.81)
AUC: 14 ng•hr/mL
P-gp substrate, but not significantly affected by P-gp inhibitors
Fecal Concentrations: 639-2710 mcg/g; OP-1118 213-1210 mcg/g
Metabolized by hydrolysis at the isobutyryl ester to form OP-1118
Metabolites: OP-1118 (active metabolite)
Enzyme substrate, inhibitor, or inducer: Not dependent on CYP450 enzymes
Half-life: 9 hr
Excretion: Feces (92%)
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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.
|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|5||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|6||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|NC||NOT COVERED – Drugs that are not covered by the plan.|
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