Indications
PO, IM, IV: Treatment of: Skin and skin structure infections,
Respiratory tract infections, Septicemia, Intraabdominal
infections, Gynecologic infections, Osteomyelitis,
Endocarditis prophylaxis. Topical: Severe acne.
Vag: Bacterial vaginosis. Unlabeled Use: PO, IM,
IV: Treatment of Pneumocystis jiroveci pneumonia,
CNS toxoplasmosis, and babesiosis.
Action
Inhibits protein synthesis in susceptible bacteria at the
level of the 50S ribosome. Therapeutic Effects:
Bactericidal or bacteriostatic, depending on susceptibility
and concentration. Spectrum: Active against
most gram-positive aerobic cocci, including: Staphylococci,
Streptococcus pneumoniae, other streptococci,
but not enterococci. Has good activity against those anaerobic
bacteria that cause bacterial vaginosis, including
Bacteroides fragilis, Gardnerella vaginalis, Mobiluncus
spp., Mycoplasma hominis, and
Corynebacterium. Also active against Pneumocystis
jirovecii and Toxoplasma gondii.
Pharmacokinetics
Absorption: Well absorbed following PO/IM administration.
Minimal absorption following topical/vaginal
use.
Distribution: Widely distributed. Does not significantly
cross blood-brain barrier. Crosses the placenta;
enters breast milk.
Protein Binding: 94%.
Metabolism and Excretion: Mostly metabolized
by the liver (by CYP3A4).
Half-life: Neonates: 3.6–8.7 hr; Infants up to 1 yr: 3
hr; Children and adults: 2–3 hr.
TIME/ACTION PROFILE (blood levels)
ROUTE ONSET PEAK DURATION
PO rapid 60 min 6–8 hr
IM rapid 1–3 hr 6–8 hr
IV rapid end of infusion
6–8 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Regional enteritis
or ulcerative colitis (topical foam); Previous
Clostridium difficile-associated diarrhea; Severe liver
impairment; Diarrhea; Known alcohol intolerance (topical
solution, suspension).
Use Cautiously in: OB: Safety not established for
topical administration; systemic administration during
2nd and 3rd trimesters not associated withqrisk of
congenital abnormalities; approved for vaginal use in
3rd trimester of pregnancy; injection contains benzyl
alcohol which can cross placenta; Lactation: Has been
used safely but appears in breast milk and exposes infant
to drug and its side effects; Pedi: Injection contains
benzyl alcohol which can cause gasping syndrome in
infants and neonates.
Adverse Reactions/Side Effects
CNS: dizziness, headache, vertigo. CV: arrhythmias,
hypotension. GI: CLOSTRIDIUM DIFFICILE ASSOCIATED DIARRHEA,
diarrhea, bitter or metallic taste, nausea, vomiting.
Derm: DRUG REACTION WITH EOSINOPHILIA AND
SYSTEMIC SYMPTOMS (DRESS), ERYTHEMA MULTIFORME,
STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS,
rash, urticaria. Local: local irritation (topical
products), phlebitis at IV site. Misc: HYPERSENSITIVITY
REACTIONS (including anaphylaxis).
Interactions
Drug-Drug: Kaolin/pectin maypGI absorption.
May enhance the neuromuscular blocking action of
other neuromuscular blocking agents. CYP3A4 inhibitors
mayqlevels. CYP3A4 inducers, including
rifampin mayplevels and lead to therapeutic failure.
Topical: Concurrent use with irritants, abrasives, or
desquamating agents may result in additive irritation.
Route/Dosage
PO (Adults): Most infections—150–450 mg every 6
hr. Pneumocystis jiroveci pneumonia—1200–1800
mg/day in divided doses with 15–30 mg primaquine/
day (unlabeled). CNS toxoplasmosis—1200–2400
mg/day in divided doses with pyrimethamine 50–100
mg/day (unlabeled); Bacterial endocarditis prophylaxis—
600 mg 1 hr before procedure.
PO (Children 1 mo): 10–30 mg/kg/day divided
every 6–8 hr; maximum dose 1.8 g/day. Bacterial endocarditis
prophylaxis—20 mg/kg 1 hr before procedure.
IM, IV (Adults): Most infections—300–600 mg
every 6–8 hr or 900 mg every 8 hr (up to 4.8 g/day IV
has been used; single IM doses of 600 mg are not recommended). P. carinii pneumonia—2400–2700
mg/day in divided doses with primaquine (unlabeled).
Toxoplasmosis—1200–4800 mg/day in divided
doses with pyrimethamine. Bacterial endocarditis
prophylaxis—600 mg 30 min before procedure.
IM, IV (Children 1mo): 25–40 mg/kg/day divided
every 6–8 hr; maximum dose: 4.8 g/day. Bacterial endocarditis
prophylaxis—20 mg/kg 30 min before
procedure; maximum dose: 600 mg.
IM, IV (Infants 1mo and 2 kg): 5 mg/kg every
8–12 hr; 2 kg—20–30 mg/kg/day divided every 6–
8 hr.
Vag (Adults and Adolescents): Cleocin, Clindamax—
1 applicatorful (5 g) at bedtime for 3 or 7 days
(7 days in pregnant patients); Clindesse—one applicatorful
(5 g) single dose; or 1 suppository (100 mg)
at bedtime for 3 nights.
Topical (Adults and Adolescents): Solution—1%
solution/suspension applied twice daily (range 1–4
times daily). Foam, gel—1% foam or gel applied once
daily.
Availability (generic available)
Capsules: 75 mg, 150 mg, 300 mg. Oral suspension:
75 mg/5 mL. Injection: 150 mg/mL. Premixed infusion:
300 mg/50 mL, 600 mg/50 mL, 900 mg/50 mL.
Topical: 1% lotion, gel, foam, solution, suspension,
single-use applicators. Vaginal cream: 2%. Vaginal
suppositories (ovules): 100 mg. In combination
with: benzoyl peroxide (Acanya, BenzaClin, Duac,
Onexton), tretinoin (Veltin, Ziana); (see Appendix B).
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