Budesonide | APOLLO | 9191 46 950 950

Budesonide | APOLLO | 9191 46 950 950

Budesonide

CAS Number : 51333-22-3

Molecular Weight : 430.534 g/mol

Molecular Formula : C25H34O6

Systematic (IUPAC) : (1S,2S,4R,8S,9S,11S,12S,13R)-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-

propyl-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icos

a-14,17-dien-16-one

DRUG DESCRIPTION

Budesonide CAS number 51333-22-3

Budesonide is a man-made glucocorticoid steroid related to the naturally-occurring hormone, cortisol or hydrocortisone which is produced in the adrenal glands.

It is used for treating asthma by inhalation. Glucocorticoid steroids such as cortisol or budesonide have potent anti-inflammatory actions that reduces inflammation and hyper-reactivity (spasm) of the

airways caused by asthma. When used as an inhaler, the budesonide goes directly to the inner lining of the

inflamed airways to exert its effects. Only 39% of an inhaled dose of budesonide is absorbed into the body, and the absorbed budesonide contributes little to the

effects on the airways

Budesonide is provided as the mixture of two epimers (22R and 22S).Budesonide is a white to off-white,

odorless powder that is practically insoluble in water and in heptane, sparingly soluble in ethanol, and freely soluble in chloroform.Its partition coefficient between

octanol and water at pH 5 is 1.6 x 10.3

USES

The budesonide inhaler is used for the control of asthma in persons requiring continuous, prolonged treatment.

Such patients may include those with frequent asthmatic episodes requiring bronchodilators.

Budesonide is used to treat Crohn's disease (a condition in which the body attacks the lining of the digestive tract, causing pain, diarrhea, weight loss, and fever).

Budesonide is in a class of medications called corticosteroids. It works by decreasing inflammation (swelling) in the digestive tract of people who have

Crohn's disease.

DOSAGE

Budesonide comes as a capsule to take by mouth. It is usually taken once a day in the morning. Take

budesonide at around the same time every day. Your doctor will tell you how long to take budesonide. Follow the directions on your prescription label carefully, and

ask your doctor or pharmacist to explain any part you do not understand. Take budesonide exactly as directed. Do

not take more or less of it or take it more often than prescribed by your doctor.

Swallow the capsules whole; do not split, chew, or crush them. If you are unable to swallow the capsules whole,

talk to your doctor.

Budesonide may help control your symptoms, but it will not cure your condition. Your doctor will watch you carefully to see how well budesonide works for you. If

your symptoms are controlled, your doctor may decrease your dose of budesonide. After your symptoms have been controlled for 3 months, your doctor may slowly decrease your dose and then stop treating you with this medication. It is important to tell your doctor how you

are feeling during your treatment.

Ask your pharmacist or doctor for a copy of the manufacturer's information for the patient.

SIDE EFFECTS

Generic Budesonide is a Corticosteroid used for the treatment of mild-to-moderately-active Crohn's disease

involving the ileum (the second half of the small intestine) and/or ascending colon (the beginning of the

large intestine). Like other medicines, Generic Budesonide can cause some side effects. If they occur, the side effects of

Generic Budesonide are most likely to be minor and temporary. However, some may be serious and need medical attention and may require the individual to

inform the doctor or visit the nearest hospital.

It is pertinent to note that side effects of Generic Budesonide cannot be anticipated. If any side effects of Generic Budesonide develop or change in intensity, the

doctor should be informed as soon as possible. Some of the most serious Generic Budesonide side

Effects include bloody or black, tarry stools, confusion, excitement, restlessness, a false sense of well being, eye pain, decreased or blurred vision, fever, sore throat,

sneezing, and cough. This is not a complete list of all Side effects. Do concur with your doctor and follow his directions completely

when you are taking Generic Budesonide.

Budesonide may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

* headache

* dizziness

* runny nose, sneezing, coughing

* nausea

* indigestion

* abdominal pain

* gas

* vomiting

* fatigue

* back pain

* pain

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately:

* itching

* skin rash

* fever

* swelling of face and neck

* difficulty breathing

* severe headache

* changes in vision

* acne

* bruising

Budesonide may cause other side effects. Call your doctor if you have any unusual problems while taking

this medication or if your symptoms get worse.

PRECAUTIONS

Before taking budesonide,

* tell your doctor and pharmacist if you are allergic to budesonide, or any other medications.

* tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the

following: clarithromycin, erythromycin, ketoconazole, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, and telithromycin. Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with budesonide, so be sure to tell your doctor about all the medications you are taking, even those that do not

appear on this list. * tell your doctor if you or anyone in your family has had diabetes (high blood sugar) or glaucoma, or if you have

tuberculosis, high blood pressure, osteoporosis (a condition in which the bones become thin and weak and break easily), stomach ulcer, cataracts, or liver disease. * tell your doctor if you are pregnant, think you may be pregnant, or plan to become pregnant, or are breast-

feeding. If you become pregnant while taking budesonide, call your doctor.

* if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking budesonide.

* tell your doctor if you have never had chicken pox or measles and you have not been vaccinated against these

infections. Stay away from people who are sick, especially people who have chicken pox or measles. If you are exposed to one of these infections or if you

develop symptoms of one of these infections, call your doctor right away. You may need treatment to protect

you from these infections.

PREPARATIONS

Pulmicort Turbuhaler 200 mcg: each 200 mcg actuation delivers 160 mcg of budesonide.

Pulmicort Respules, 0.25 mg/2ml, 0.5 mg/2ml suspension, and 1 mg/2ml

STORAGE

Budesonide should be stored at room temperature, 20-25 C (68-77 F).

PRESCRIBED FOR: The budesonide inhaler is used for the control of asthma in persons requiring continuous, prolonged treatment. Such patients may include those

with frequent asthmatic episodes requiring bronchodilators, for example, albuterol (Ventolin) or

those with asthmatic episodes at night.

DOSING

Budesonide is used to prevent asthmatic attacks and should not be used to treat an acute attack of asthma.

The Turbuhaler is used for individuals six years of age or older. Effects can be seen within 24 hours, but

maximum effects may not be seen for 1-2 weeks or longer. Doses vary widely. Adults usually receive 1 to 4 actuations (puffs) twice daily. Children usually receive 1

to 2 puffs twice daily. For those with mild asthma, treatment once daily may be sufficient.

Pulmicort Respules are used for individuals 12 months to eight years of age. Effects are seen in 2 to 8 days, but maximum effects may not be seen for up to 4 to 6 weeks. Pulmicort Respules are used with a jet nebulizer. They usually are taken as one or two doses for a total of 0.5-1

mg daily.

DRUG INTERACTIONS

Ketoconazole (Nizoral, Extina, Xolegel, Kuric) increases the concentrations in blood of budesonide, and this may lead to an increase in the side effects of budesonide. No drug interactions have been described with inhaled

budesonide.

PREGNANCY

When given orally to animals, glucocorticoid steroids similar to budesonide have been shown to cause fetal

abnormalities. Studies of pregnant women using inhaled budesonide during early pregnancy, however, do not show an increase in the rate of fetal abnormalities. Nevertheless, since these studies cannot exclude the

possibility of rare effects on the fetus, inhaled budesonide should be used with caution during

pregnancy.

NURSING MOTHERS

It is not known if budesonide is secreted in breast milk. Other medications similar to budesonide are indeed secreted in breast milk. It is not known whether the small amounts that may appear in breast milk have

effects on the infant.

Type

small molecule

Description

A glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis.

Categories

Anti-inflammatory Agents

Bronchodilator Agents

Corticosteroids

Glucocorticoids

Pharmacology

Indication

For the treatment of mild to moderate active Crohn's disease. Also for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for

treatment and prevention of nasal polyposis.

Pharmacodynamics

Budesonide is a synthetic corticosteroid used in Crohn's disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare

up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution in gastric juice, but which dissolve at

pH >5.5, ie, normally when the granules reach the duodenum. Thereafter, a matrix of ethylcellulose with budesonide controls the release of the drug into the

intestinal lumen in a time-dependent manner.

Mechanism of action

The exact mechanism of action of budesonide in the treatment of Crohn's disease is not fully understood.

However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect.

Absorption

Absorption is complete following oral administration.

Metabolism

Following absorption, budesonide is subject to high first pass metabolism (80-90%). In vitro experiments in

human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by

CYP3A4, to its 2 major metabolites, 6b-hydroxy budesonide and 16a- hydroxy prednisolone. The

glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.

Route of elimination

Budesonide is excreted in urine and feces in the form of metabolites.

Toxicity

Single oral doses of 200 and 400 mg/kg were lethal in female and male mice, respectively. The signs of acute toxicity were decreased motor activity, piloerection and

generalized edema.

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