Methylprednisolone

BRAND NAMES:

Medrol - It contains the active ingredients of methylprednisolone. It is available in the form of tablets used to treat allergic conditions and inflammation in the body.

Medrol Dosepak – it contains the active ingredient of methylprednisolone. It is available in the form of tablets used to treat any type of inflammation.

Depo Medrol- It contains the active ingredient of methylprednisolone. It is available in the form of an injection. Also, it is available with a combination of lidocaine.

Hybrisil - It contains the active ingredients of methylprednisolone. It is available in the form of gel used to treat topical scar treatment.

MECHANISM OF ACTION:

Methylprednisolone also suppresses the synthesis of cyclooxygenase -2, an enzyme that produces prostaglandins in damaged tissue and contributes to the inflammation cascade. Through these actions, methylprednisolone can reduce or prevent inflammation by reversing capillary permeability, suppressing the migration of fibroblast and polymorphonuclear leukocytes, controlling the rate of protein synthesis, and stabilizing lysosomes at the cellular level.

PHARMACOKINETICS:

Absorption: Methylprednisolone has rapid and linear absorption, reaching peak concentrations 48 minutes after administration. The action of intravenous methylprednisolone succinate begins within an hour. Intra-articular methylprednisolone acetate has an onset of action of 1 week and a duration of 1-5 weeks. Methylprednisolone has an oral bioavailability of about 88 percent.

Distribution: Methylprednisolone succinate has a volume of distribution of 24±6 L and a steady-state volume of distribution of 27±8.2 L. This drug primarily binds to albumin in plasma. 

Metabolism: Methylprednisolone undergoes hepatic metabolism to produce metabolites such as 20-carboxymethylprednisolone.

 Excretion: Methylprednisolone is primarily excreted in urine, following a bi-exponential pattern. The half-life elimination of intravenous methylprednisolone is 0.25 hours, with an oral half-life of 2-5 hours.

PHARMACODYNAMICS:

Patients taking corticosteroids should be advised about the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infection. Corticosteroids bind to the glucocorticoid receptor, reducing pro-inflammatory signals and increasing anti-inflammatory signals. Corticosteroids have a broad therapeutic window because patients may require doses that exceed what the body naturally produces. 

DOSAGE AND ADMINISTRATION:

Methylprednisolone is available and has the following strengths

Tablets- 2mg, 4mg, 8mg, 16mg and 32mg

Injectable suspensions- 20mg/ml, 40mg/ml, and 80mg/ml

Power of injection – 40mg, 125mg, 500mg, 1gr and 2gr

Methylprednisolone is available in tablet form for oral administration. Do not stop taking methylprednisolone without consulting your doctor. Stopping the drug abruptly can result in loss of appetite, nausea, vomiting, drowsiness, confusion, headache, fever, joint and muscle pain, peeling skin, and weight loss. If you have been taking large doses for an extended period, your doctor will most likely gradually reduce your dose to allow your body to adjust before discontinuing the drug completely. 

DRUG INTERACTIONS:

Drug interactions of Methylprednisolone may include

• Tuberculosis drugs– rifampicin and isoniazid

• Blood thinner medicines– aspirin and warfarin

• Anti-epilepsy drugs- carbamazepine, phenobarbital and phenytoin

• Anticholinergics medicine – amitriptyline

• Antidiabetic drugs – insulin

• HIV medications – cobicistat

• NSAIDs – ibuprofen, naproxen

• Diuretics – thiazides, furosemide and ethacrylic acid

• Asthma medicines – theophylline, salbutamol, salmeterol

• Fungal infection medicines- amphotericin B

CONTRAINDICATIONS:

Methylprednisolone should not be used if you have a documented hypersensitivity to the medication or its components, or if you have systemic fungal infection. Other glucocorticoids, including methylprednisolone, should be used with extreme caution in people who have peptic ulcers, heart disease or hypertension with heart failure, certain viral infections like varicella and tuberculosis, psychoses, diabetes, osteoporosis, or glaucoma.

SIDE EFFECTS:

Methylprednisolone may cause side effects

• Upset stomach

• Stomach irritation

• Vomiting

• Headache

• Dizziness

• Insomnia

• Restlessness

• Depression

• Anxiety

• Acne

• Easy bruising

• Irregular menstrual periods

OVERDOSE:

Overdose of the drug leads to some side effects as below

• High blood pressure

• Swelling of your arms, legs or feet

• Weakness

• Tiredness

• Muscle cramps

TOXICITY:

Treat acute overdose with symptomatic and supportive therapy while chronic overdoses will require temporarily reduced dosages.