⚡ Quick Answer — What is Unicontin-E?
Unicontin-E bevat theophylline, een methylxanthine bronchodilator with anti-inflammatory effects, used as add-on therapy for chronic asthma and COPD. Theophylline acts on multiple targets — phosphodiesterase inhibition (raising cAMP), adenosine receptor antagonism, and HDAC2 activation (anti-inflammatory). It has a narrow therapeutic index (target serum 10–20 mg/L; toxicity at 20+) and many drug interactions, requiring careful dosing and (in some patients) blood-level monitoring. Each controlled-release tablet contains 400 mg, geproduceerd door Modi-Mundipharma in WHO-GMP gecertificeerde faciliteiten.
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What Is Unicontin-E?
Unicontin-E is an oral methylxanthine bronchodilator. Methylxanthines are derived from natural alkaloids (theophylline is the dimethylxanthine present in tea). Their use has declined since the 1990s as inhaled β2-agonists and corticosteroids became first-line — but they retain a role as third-line add-on therapy in difficult asthma and COPD.
How Does Unicontin-E Work?
- Phosphodiesterase inhibition (PDE3, PDE4) — raises cyclic AMP in airway smooth muscle and inflammatory cells; net result is bronchodilation and reduced mediator release.
- Adenosine receptor antagonism — blocks adenosine-mediated bronchoconstriction and mast-cell mediator release.
- HDAC2 activation (theophylline at low serum levels 5–10 mg/L) — restores corticosteroid responsiveness in COPD and severe asthma where steroid resistance is partly mediated by reduced HDAC2.
- Diaphragm contractility — methylxanthines reduce diaphragm fatigue, useful in COPD with severe airflow limitation.
Toepassingen en Indicaties
- Severe chronic asthma — add-on to high-dose ICS-LABA where additional bronchodilation is needed
- COPD maintenance — add-on to LAMA-LABA or triple therapy
- Nocturnal asthma — sustained-release formulation provides overnight bronchodilation
- Apnoea of prematurity (theophylline) — neonatal use
- Cor pulmonale and pulmonary hypertension — adjunct
Unicontin-E Dosage
| Patiënt | Dosering | Frequentie |
|---|---|---|
| Adults — initial | 200 mg | Twice daily; titrate to serum level 10–20 mg/L |
| Adults — maintenance | 400 mg | Twice daily (or 600 mg once daily ER) |
| Elderly / heart failure / liver disease | Halve dose | Monitor serum level |
Side Effects of Unicontin-E
- Nausea, vomiting, dyspepsia
- Hoofdpijn
- Tremor
- Insomnia, restlessness
- Tachycardia, palpitations
- Mild hypokalaemia at high doses
Toxic levels (>20 mg/L) — emergency:
- Severe nausea, persistent vomiting
- Cardiac arrhythmia (atrial fibrillation, supraventricular tachycardia)
- Seizures (often without warning)
- Hypotension, hyperglycaemia, hypokalaemia, hypercalcaemia
Waarschuwingen en voorzorgsmaatregelen
- Narrow therapeutic index. Target serum 10–20 mg/L. Check blood level 5 days after starting, after dose change, with new interacting drug, with smoking cessation, and during illness/fever (clearance falls).
- Many drug interactions — see interactions table. Most metabolised by CYP1A2; many inhibitors and inducers shift levels significantly.
- Smoking induces CYP1A2 and lowers theophylline levels by ~50% — re-titrate at smoking cessation.
- Cardiac disease: use cautiously in arrhythmias, heart failure, severe hypertension.
- Hyperthyroidism: increased clearance plus exaggerated adrenergic effects.
- Zwangerschap en borstvoeding: generally avoided; use only if benefit clear.
- Liver disease: reduce dose — methylxanthines are hepatically metabolised.
Contra-indicaties
- Hypersensitivity to theophylline or other xanthines (caffeine, theobromine)
- Actieve maagzweer
- Uncontrolled tachyarrhythmias
- Severe heart failure (NYHA IV)
Geneesmiddelinteracties
| Interagerend geneesmiddel | Effect | Wat te doen |
|---|---|---|
| Ciprofloxacin, erythromycin, clarithromycin, fluvoxamine | Inhibit CYP1A2 → raise theophylline levels → toxicity (nausea, arrhythmia, seizures) | Avoid or reduce theophylline dose 50%; check serum levels |
| Cimetidine, allopurinol | Raise theophylline levels | Reduce dose; monitor levels |
| Phenytoin, carbamazepine, rifampicin | Induce CYP — lower levels | Higher dose may be needed |
| Smoking | Induces CYP1A2 — lower levels | Re-titrate dose at smoking cessation |
| β-agonists, diuretics | Additieve hypokaliëmie | Monitor potassium |
Opslag
- Bewaren beneden 25°C in a cool, dry place away from direct sunlight.
- Keep in original packaging until use to protect from moisture and light.
- Do not use after the expiry date printed on the strip.
- Buiten bereik van kinderen houden.
Gerelateerde alternatieven op MedsBase
- Asthalin Inhaler — salbutamol verlichter
- Budecort Inhaler — budesonide ICS-preventer
- Foracort Inhaler — budesonide + formoterol ICS-LABA
- Tiova Inhaler — tiotropium LAMA voor COPD
- Montair — montelukast LTRA-tablet
Veelgestelde vragen
Is theophylline still used in modern asthma management?
Yes, but as third-line add-on. Inhaled β2 agonists, ICS, ICS-LABA, LTRA, and LAMA are first-line; theophylline is added for refractory disease, particularly nocturnal asthma. The narrow therapeutic index and many drug interactions limit its use.
How is the dose decided?
Adjusted to serum theophylline level 10–20 mg/L. Check 5 days after starting, after dose change, with new interacting drug, with smoking cessation, and during illness/fever.
Why so many interactions?
Theophylline is metabolised by CYP1A2 — many drugs raise levels (ciprofloxacin, erythromycin, fluvoxamine, cimetidine) or lower levels (rifampicin, phenytoin, smoking).
How long does Unicontin-E last?
The controlled-release tablet provides 12-hour cover. Twice-daily dosing maintains stable serum levels.
What are the toxic symptoms?
Severe nausea, persistent vomiting, tachycardia, palpitations, tremor, hyperactivity, seizures (often without warning), arrhythmias, hypotension. Toxicity above 20 mg/L is an emergency — withhold dose, check level, supportive care.
Can I take it with caffeine?
Caffeine and theophylline are both methylxanthines with overlapping effects. Heavy caffeine can amplify tremor, tachycardia, and insomnia. Reduce caffeine if symptomatic.
Why does smoking affect dose?
Smoking induces CYP1A2 (the enzyme that metabolises theophylline). Smokers need higher doses; on stopping, levels rise — re-titrate.
Is Unicontin-E safe in pregnancy?
Generally avoided unless benefit clear. Inhaled therapy is preferred.
Can I crush or split Unicontin-E tablets?
No — controlled-release tablets must be swallowed whole. Crushing destroys the release matrix and risks acute toxicity.
Gerelateerde alternatieven
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