Opill
Opill
Generic Name
Opill
Mechanism
- Selective COX inhibition:
- COX‑1 & COX‑2 inhibition reduces prostaglandin synthesis.
- Reduction of inflammation, pain, and fever:
- Decreases synthesis of PGE₂ and PGI₂, attenuating pain pathways and interrupting hyperthermia.
- Therapeutic window:
- Relatively short plasma half‑life allows for pulsatile dosing with minimal accumulation in most patients.
---
Pharmacokinetics
- Absorption: Rapid; peak plasma levels (~1 h post‑dose) when taken on an empty stomach.
- Bioavailability: ~80 % orally; food delays absorption by ~30 min but does not affect extent.
- Distribution: Widely distributed; protein binding ~99 % (mostly to albumin).
- Metabolism: Hepatic via CYP2C9 and CYP3A4 → primarily inactive glucuronide conjugates.
- Elimination: Renal excretion (~20 % unchanged; 80 % metabolite).
- Half‑life: ~2 – 3 h (steady state reached after 3–4 d of regular dosing).
- Drug interactions:
- CYP2C9 inhibitors (e.g., fluconazole) ↑ ibuprofen levels.
- Other NSAIDs → additive GI or renal toxicity.
- Anticoagulants → ↑ bleeding risk.
---
Indications
- Analgesia:
- Post‑operative pain, dental pain, dysmenorrhea.
- Antipyretic: Managing fever (e.g., influenza, common cold).
- Anti‑inflammatory: Mild rheumatoid arthritis flares, osteoarthritis pain.
---
Contraindications
| Category | Key Points |
| Absolute contraindications |
• Known hypersensitivity to ibuprofen or other NSAIDs. |
| Relative |
• Active peptic ulcer disease, severe gastritis.
• Uncontrolled hypertension, congestive heart failure (NYHA II–IV).
• Severe renal impairment (CrCl < 30 mL/min).
• Hepatic failure.
• Elderly patients ≥ 65 yr (increased GI bleeding risk). |
| Pregnancy & Lactation |
• Avoid in 3rd trimester; only use after 36 wk if essential.
• Breastfeeding: minimal excretion; safe if < 200 mg/d. |
| Misc. |
• Use with caution in patients on anticoagulants or antiplatelet therapy. |
--
•
Dosing
| Population | Dose | Frequency | Total Daily Limit |
| Adult & Adolescents (≥ 12 yr) | 200 mg per tablet | Every 6‑8 h as needed | ≤ 1200 mg/day (6 tablets) |
| Elderly (≥ 65 yr) / Renal ↓ | Reduce dose | 200 mg every 8‑12 h | ≤ 800 mg/day if CrCl 30–60 mL/min |
| Children (12‑18 yr) | 5–10 mg/kg/dose | Every 6‑8 h | Max 40 mg/kg/24 h |
| Hyper‑thermia/Severe Pain | 400 mg/2 tablets | 6 h interval | ≤ 1200 mg/day |
• Administration: Oral, with or without food; food reduces GI irritation.
• Missed dose: If within 30 min, take. Otherwise skip; do not double dose.
• Switching to other NSAIDs: Provide 24‑hr washout to avoid cumulative toxicity.
--
•
Adverse Effects
| System | Common Adverse Effects | Serious Adverse Effects |
| Gastrointestinal | Nausea, dyspepsia, epigastric pain | Peptic ulcer, GI bleeding, perforation |
| Renal | Mild proteinuria, transient azotemia | Acute interstitial nephritis, renal failure |
| Cardiovascular | Mild palpitations, headache | Hypertension, fluid retention, heart failure exacerbation |
| Central nervous system | Headache, dizziness | Severe CNS depression (rare) |
| Haematologic | Mild thrombocytopenia | Severe thrombocytopenia, pancytopenia |
| Allergic | Rash, pruritus | Anaphylaxis, angioedema |
--
•
Monitoring
| Parameter | Frequency | Rationale |
| CBC & platelets | Baseline; repeat 2–4 weeks if on > 4 weeks therapy | Detect thrombocytopenia |
| Serum creatinine & BUN | Baseline; repeat 1 month after starting; monthly thereafter in at-risk patients | Monitor renal function |
| Liver enzymes (ALT/AST) | Baseline; repeat 1 month after start | Detect hepatotoxicity |
| Blood pressure | Baseline; every visit in patients with hypertension | NSAIDs can raise BP |
| Symptom check for GI bleeding | Continuous | Early detection of ulceration or hemorrhage |
--
•
Clinical Pearls
- “Two‑tablet rule”: Taking two tablets (400 mg) rapidly raises plasma concentration → potentiate analgesia but also increases GI risk. Use sparingly.
- Gastric protection: For patients at risk, prescribe a proton‑pump inhibitor (e.g., omeprazole 20 mg qd).
- Kidney safety: Monitor serum creatinine in patients on ACE inhibitors/ARBs; consider dose adjustment if GFR falls < 30 mL/min.
- Pregnancy caution: If symptomatic relief is needed, consider acetaminophen first; if NSAID required, defer until after 36 growth weeks.
- Drug Drug interactions: Avoid concomitant use of *digoxin*; NSAIDs may raise digoxin levels.
- Elderly dosing: Start at the lower end (200 mg) and titrate based on pain relief and tolerance.
- Food & Timing: Gastric irritation is minimized when Opill is taken with a full meal or milk.
--
• Opill remains a cornerstone analgesic for acute pain and fever when used judiciously, with vigilant monitoring for GI, renal, and cardiopulmonary complications.