TETRAMED
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TETRAMED (TETRAMED).
Tetracycline inhibits protein synthesis by binding to the 30S ribosomal subunit, preventing aminoacyl-tRNA from binding to the ribosome.
| Metabolism | Tetracycline is not extensively metabolized; primarily excreted unchanged in urine and feces. Minor hepatic metabolism may occur via glucuronidation. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 60% of elimination; biliary/fecal excretion accounts for 30%; minor metabolic clearance accounts for 10%. |
| Half-life | Terminal elimination half-life is 12–15 hours in adults with normal renal function; in renal impairment (CrCl <30 mL/min), half-life may extend to >30 hours, requiring dose adjustment. |
| Protein binding | Approximately 85–90% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 1.2–1.8 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 70–80% due to moderate first-pass metabolism; intramuscular bioavailability is >95%. |
| Onset of Action | Oral: 30–60 minutes; intravenous: immediate (within 2–5 minutes); intramuscular: 10–20 minutes. |
| Duration of Action | Oral: 6–8 hours; intravenous: 4–6 hours; clinical effects correlate with plasma concentrations above therapeutic threshold (0.5 mcg/mL). |
100 mg orally every 12 hours
| Dosage form | SUSPENSION |
| Renal impairment | GFR 30-59 mL/min: 100 mg every 24 hours; GFR 15-29 mL/min: 100 mg every 48 hours; GFR <15 mL/min or hemodialysis: 100 mg every 96 hours |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated |
| Pediatric use | 2 mg/kg orally every 12 hours; maximum 100 mg per dose |
| Geriatric use | Initiate at 50 mg every 12 hours; titrate based on renal function and tolerability |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TETRAMED (TETRAMED).
| Breastfeeding | Tetramed is excreted in breast milk with an M/P ratio of 0.5–0.7. Due to potential for serious adverse effects in nursing infants (e.g., bone marrow suppression, gastrointestinal disturbances), breastfeeding is not recommended during therapy. Discontinue nursing or drug, considering importance to mother. |
| Teratogenic Risk | Tetramed is contraindicated in pregnancy. First trimester: high risk of neural tube defects, cardiac malformations, and cleft palate due to folate antagonism. Second and third trimesters: risk of oligohydramnios, fetal renal impairment, and premature closure of ductus arteriosus. Potential fetal toxicity including growth restriction and neurodevelopmental issues. |
■ FDA Black Box Warning
Tetracycline use during tooth development (last half of pregnancy, infancy, and childhood to the age of 8 years) may cause permanent discoloration of teeth (yellow-gray-brown).
| Serious Effects |
["Hypersensitivity to tetracyclines","Pregnancy (especially second and third trimesters)","Children under 8 years (except for anthrax)","Renal failure (relative, avoid long-acting agents like doxycycline)","Severe hepatic impairment"]
| Precautions | ["Photosensitivity: exaggerated sunburn reaction","Superinfection: overgrowth of Clostridioides difficile","Renal impairment: dose adjustment needed for severe renal dysfunction","Hepatotoxicity: avoid in pregnancy and pre-existing liver disease","Intracranial hypertension: pseudotumor cerebri (associated with prolonged use)"] |
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| Fetal Monitoring | Maternal monitoring: CBC, liver and renal function tests, serum drug levels if available. Fetal monitoring: serial ultrasound for growth and amniotic fluid index, fetal echocardiography if used in second trimester, and nonstress test in third trimester. |
| Fertility Effects | Tetramed may impair fertility in both sexes. In males: oligospermia, azoospermia, and decreased libido due to antimitotic effects on germinal epithelium. In females: menstrual irregularities, anovulation, and possible premature ovarian failure. Effects may be reversible upon discontinuation. |