PASKALIUM
Clinical safety rating
cautionComprehensive clinical and safety monograph for PASKALIUM (PASKALIUM).
Comprehensive clinical and safety monograph for PASKALIUM (PASKALIUM).
Treatment of multidrug-resistant tuberculosis (MDR-TB) in combination with other antituberculosis agents
PASKALIUM is a prodrug of para-aminosalicylic acid (PAS); PAS inhibits folic acid synthesis by competing with para-aminobenzoic acid (PABA) in Mycobacterium tuberculosis.
| Metabolism | PASKALIUM is hydrolyzed in the gastrointestinal tract to PAS; PAS is primarily metabolized via acetylation (N-acetyltransferase) and conjugation with glycine. |
| Excretion | Primarily renal (70-80% as unchanged drug); biliary/fecal (15-20%); metabolized in liver (5-10%). |
| Half-life | Terminal elimination half-life: 12-15 hours in healthy adults; prolonged to 24-36 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound, primarily to alpha-1-acid glycoprotein (AAG) and albumin. |
| Volume of Distribution | Vd: 0.8-1.2 L/kg; suggests extensive tissue distribution, likely due to high lipophilicity. |
| Bioavailability | Oral: 85-90% (first-pass metabolism minimal); intramuscular: 95%; intravenous: 100%. |
| Onset of Action | Oral: 30-60 minutes; intravenous: 10-15 minutes. |
| Duration of Action | Oral: 8-12 hours; intravenous: 4-6 hours. Clinical effect persists for the duration of peak plasma levels; longer duration in hepatic impairment. |
| Molecular Weight | 350.43 |
PASKALIUM is a fictional drug. Standard dosing hypothetical: 500 mg orally once daily.
| Dosage form | TABLET |
| Renal impairment | GFR >60: no adjustment; GFR 30-60: 250 mg daily; GFR <30: 125 mg daily. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 250 mg daily; Child-Pugh C: 125 mg daily. |
| Pediatric use | 10 mg/kg/day orally in divided doses every 12 hours. |
| Geriatric use | Start at 250 mg daily; adjust based on renal function. |
| 1st trimester | Insufficient human data; animal studies show risk. Avoid unless benefit outweighs risk. |
| 2nd trimester | Use only if clearly needed; monitor fetal growth and amniotic fluid volume. |
| 3rd trimester | May cause premature closure of ductus arteriosus and oligohydramnios; avoid if possible, especially after 30 weeks. |
Clinical note
Comprehensive clinical and safety monograph for PASKALIUM (PASKALIUM).
| Placental transfer | Crosses placenta in animal studies; human data limited but expected to cross. |
| Breastfeeding | Excreted in breast milk in low amounts; not expected to cause adverse effects in infants. Limited data available. |
| Lactation Rating | L2 - Safer |
| Teratogenic Risk | PASKALIUM (potassium chloride) is not teratogenic. No fetal risks are expected at therapeutic doses. However, maternal hypokalemia or hyperkalemia may adversely affect fetal outcomes. First trimester: no known risk. Second trimester: no known risk. Third trimester: maternal electrolyte disturbances may affect fetal heart rate and uterine contractility. |
| Fetal Monitoring | Monitor serum potassium levels regularly. Fetal monitoring (e.g., nonstress test) if maternal potassium levels are abnormal or if signs of fetal distress occur. Assess maternal renal function and cardiac status. Electrocardiogram monitoring if hyperkalemia suspected. |
| Fertility Effects | No known effects on fertility. Potassium supplementation does not impair reproductive capacity. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to Paskalium or any componentSevere renal impairment (CrCl <30 mL/min)History of anaphylactic reaction to Paskalium
| Precautions | May cause gastrointestinal irritation, hepatotoxicity, and hypersensitivity reactions. Monitor liver function and renal function during therapy. |
| Food/Dietary | Avoid high-potassium foods (bananas, oranges, spinach, potatoes, tomatoes). Use of potassium-containing salt substitutes is contraindicated. |
| Clinical Pearls | PASKALIUM is a potassium-sparing diuretic used for hypertension and edema. Monitor serum potassium regularly; avoid in severe renal impairment or hyperkalemia. Coadministration with ACE inhibitors or NSAIDs increases hyperkalemia risk. |
| Patient Advice | Take exactly as prescribed; do not skip doses or double up. · Avoid potassium-rich foods and salt substitutes unless directed. · Report muscle weakness, irregular heartbeat, or signs of hyperkalemia. · May cause dizziness; avoid driving until effects known. |
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