舒噻嗪(Ospolot)的详细说明书：作用与功效,用法用量,副作用,注意事项等

Author: Medicalhalo

Release time: 2025-10-19 11:44:20

Ospolot is a sulfonamide derivative anti-epileptic drug with no structural similarity to other anti-convulsant drugs.

Ospolot indications

It is used to treat persistent spike-and-wave syndrome (POCS) during sleep, after failure of existing and appropriate treatment options.

Ospolot usage and dosage

1. Dosage

The maintenance dose is approximately 5 to 10 mg/kg body weight per day. This dose should be achieved gradually and in stages over one to two weeks, or treatment can be started with a maintenance dose.

2. How to take it

The daily dose should be taken in three divided doses as much as possible. With this daily dosing, stable blood levels will be achieved within five to six days.

Film-coated tablets should be taken whole with water (about a cup of water) and should not be chewed.

3. Duration of use

The duration of use depends on the individual response of the patient. If treatment is unsuccessful, treatment with albumethazine should be stopped after approximately one month.

Sutiazide should not be stopped suddenly, discontinuation can be completed quickly within one to two weeks.

The pictures come from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Contraindications of Ospolot

Absolute contraindications

1. Known allergy to Ospolot, other sulfa drugs or any excipients.

2. Renal insufficiency.

3. Have a history of mental illness.

4. Porphyria.

5. Hyperthyroidism.

6. Untreated hypertension.

Ospolot Precautions

1. Once bone marrow suppression or allergic rash occurs, Ospolot must be stopped immediately. Therefore, patients are advised to seek immediate medical attention and undergo routine blood tests if they develop fever, sore throat, rash, and/or swollen lymph nodes, with or without flu-like symptoms.

2. For long-term treatment, blood routine and renal function parameters should be monitored regularly. It is recommended that a check-up be performed before starting treatment with alfamethiazide, then weekly for the first month of treatment, and then monthly thereafter. After six months of treatment, two to four checkups per year will suffice.

3. Progressive thrombocytopenia or leukopenia, usually accompanied by clinical symptoms such as fever or sore throat, requires interruption of treatment.

4. If serum creatinine continues to rise, treatment must also be interrupted.

5. If severe allergic reaction occurs, albutiazide must be stopped immediately.

6. Suicidal thoughts and behaviors have been reported in patients receiving anti-epileptic drugs for different indications. A meta-analysis of randomized, placebo-controlled studies of antiepileptic drugs also showed a slightly increased risk of suicidal thoughts and behaviors. The mechanism of this adverse effect has not been established and available data cannot exclude the possibility that use of albumethane may increase this risk.

7. Patients should be monitored for any signs of suicidal thoughts and behaviors, and appropriate treatment should be considered. Patients (and their caregivers) should be advised to seek medical help if they experience signs of suicidal thoughts or behaviors.

8. Suthiazine contains lactose and is not recommended for patients with galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome (rare genetic diseases).

Ospolot drug interactions

1. The effect of Ospolot on the plasma concentration of other drugs

Ospolot is an inhibitor of CYP2C isoenzyme and may increase the plasma concentration of other drugs through this mechanism. Therefore, the effects of certain other drugs that are degraded by the same enzymes may be enhanced and toxic effects may be observed when taken concomitantly.

When coadministered with sulfamethoxazole, the dose of the following active ingredients may need to be reduced if necessary: phenytoin, barbiturates, diazepam, imipramine, diclofenac, ibuprofen, naproxen, warfarin, omeprazole, proguanil, propranolol, retinol and tolbutamide.

2. Drugs that may reduce the plasma concentration of suthiazide

Phenobarbital, phenytoin, primidone and carbamazepine may reduce the plasma concentration of suthiazide.

Due to the possibility of interactions, especially when multiple antiepileptic drugs are used concurrently, it is recommended to monitor plasma concentrations and adjust the dose of alfamethiadine if necessary.

Ospolot medication for special populations

Pregnancy and lactation

Experimental studies have proven that Ospolot is embryotoxic, and any potential risks to humans are unclear. There are no available data on use in human pregnancy or lactation. Use of albumethane during pregnancy and lactation is not recommended.

Adverse reactions of Ospolot

The following side effects may occur depending on the dose, especially at the beginning of treatment:

1. Respiratory system, chest and mediastinal diseases

Common: shortness of breath, hyperpnea or dyspnea, especially at the beginning of treatment: hiccups (this symptom will subside on its own in 1 to 2 weeks in most cases, or will subside after temporarily reducing the dose; it can be prevented by gradually increasing the dose).

2. Blood and lymphatic system diseases

Very rare: leukopenia, granulocytopenia, neutropenia, thrombocytopenia.

3. Gastrointestinal diseases

Very common: stomach pain, especially in the early stages of treatment.

Common: Nausea and vomiting. These symptoms will in most cases resolve on their own within 1 to 2 weeks or with a temporary dose reduction, and can be prevented by gradually increasing the dose.

4. Hepatobiliary system diseases

Very rare: hepatotoxic reaction, elevated liver enzymes.

5. Metabolic and nutritional disorders

(1) Common: loss of appetite, especially in the early stages of treatment. (In most cases resolves spontaneously within 1 to 2 weeks, or resolves after a temporary dose reduction; may be prevented by gradually increasing the dose.) Weight loss.

(2). Very rare: metabolic acidosis. When metabolic acidosis occurs, compensatory hyperventilation may occur.

6. Musculoskeletal and connective tissue diseases

Uncommon: joint pain and muscle weakness.

7. Skin and subcutaneous tissue diseases

(1). Rare: rash.

(2) Unknown frequency: Stevens-Johnson syndrome or Lyell syndrome, DRESS syndrome or anaphylaxis.

8. Heart disease

Common: angina pectoris, tachycardia.

9. Vascular diseases

Unknown frequency: blood pressure increases or decreases.

10. Nervous system diseases

(1) Common: abnormal sensation in limbs and face, dizziness, headache, especially in the early stage of treatment. (These symptoms will subside on their own in 1 to 2 weeks in most cases, or will subside after temporarily reducing the dose. They can be prevented by gradually increasing the dose.)

(2) Uncommon: Difficulty thinking. Muscle weakness. Grand mal seizure state or increased frequency of seizures.

(3), unknown frequency: polyneuritis.

11. Mental illness

(1) Uncommon: confusion or even agitation, especially in the early stages of treatment. In most cases these symptoms will resolve on their own within one to two weeks or with a temporary dose reduction. It can be prevented by gradually increasing the dose. Hallucinations, anxious states, or lack of motivation.

(2) Unknown frequency: behavioral disorders, such as aggression, irritability, and mood disorders. Underlying psychosis may be activated by treatment with albumethazine.

12. Eye diseases

Common: diplopia.

13. Kidney and urinary system diseases

Rare: renal failure and urinary retention.

14. Reproductive system and breast diseases

Rare: impotence.

Mechanism of action of Ospolot

Suthiazine is a sulfonamide derivative with no structural similarity to other anticonvulsants. Its mechanism of action has not yet been fully elucidated. The best documented biological effect is inhibition of central carbonic anhydrase, and effects on excitatory and inhibitory neurotransmitter homeostasis have also been described.

In addition, albutarine reduces the entry of sodium ions into neurons, thereby lowering their excitability threshold. The antiepileptic effects of sulfamethoxazine have been demonstrated in convulsions induced by electroshock (rats and mice) or pentylenetetrazole (mice).

The anticonvulsant effects of albutiazide may reduce convulsive seizures in children with Rolando epilepsy (a benign childhood epilepsy with centrotemporal spikes).

Ospolot Pharmacokinetics

1. Absorption

After oral administration, Ospolot is rapidly and almost completely absorbed in the upper small intestine. The effect of food on the absorption of albutarine has not been studied. The oral bioavailability of albumethazine has also not been studied.

2. Distribution

Plasma concentration reaches its peak within 1 to 5 hours. Despite linear pharmacokinetics, there are large intra- and inter-individual fluctuations in plasma concentrations even after steady state is achieved. Therapeutic and toxic plasma concentrations have not yet been determined. Plasma concentrations of 1 to 6 µg/ml of alfamethiazide are achieved after administration of approximately 5 mg/kg body weight.

The binding rate of albutiazide to plasma proteins is approximately 29%.

3. Metabolism

Two metabolites of albutiazine have been identified in human urine. The quantitatively most important metabolite is hydroxysulthiazine, which has no anticonvulsant activity.

4. Elimination

The half-life of albutiazine is between 2 and 16 hours. The half-life is shorter when combined with enzyme-inducing antiepileptic drugs than when used alone. After oral administration, 80% to 90% of the dose is excreted via the kidneys and 10% to 20% is excreted in the feces via bile secretion. About 30% is excreted unchanged through the kidneys within 24 hours. More than 25% of the product is excreted as a metabolite (hydroxysulfinate).