Medical  Explorer

Custom Search

Drugs A to Z  :  A  B  C  D  E  F  G  H  I  J  K  L  M  N  O  P  R  S  T  U  V  W  X  Y  Z
Medicinal Ingredients : A  B  C  D  E  F  G  H  I  J  K  L  M  N  O  P  Q  R  S  T  U  V  W  X  Y  Z

Beauty Products : A  B  C  D  E  F  G  I  M  N  O  P  R  S  T  V

Aging      Allergies     Alzheimer's      Arthritis    Asthma      Bacteria   new Cancer    Chickenpox     Colds     Constipation      Diabetes      Epilepsy     Fatigue     Fever     Genetics       Haemorrhoids       newHeadaches      Hepatitis    Immunity      Infection      Insomnia       Leprosy       Menopause      Obesity      Osteoporosis     Other Diseases    Pain      PMS     Parasites     Sinusitis     newStroke     Toxicology    Urology




Arthritis medications
Acupuncture
Alcohol
Patients
newGeneral Health
Medicinal food
Chinese medicine
Nutrients
Smoking
Vitamins
OTC Drugs
Health Products
Therapy
Symptom
Parasitology
 
 

Depo-Medrol

METHYLPREDNISOLONE ACETATE

Sterile aqueous suspension


Composition
DEPO-MEDROL Sterile aqueous suspension 40 mg per ml

Each ml contains:
Methylprednisolone acetate 40 mg.


Forms, ways of administration and packages
FORM: sterile aqueous suspension for single use.

WAYS OF ADMINISTRATION
- Intramuscular
- Intra-articular, periarticular, intrabursal or soft tissues
- Intralesional
- Intrarectal instillation


DEPO-MEDROL is contra-indicated for I.V. administration. DEPO-MEDROL is not recommended for intrathecal, epidural, intranasal, intra-ocular or any other unapproved route of administration (see ADVERSE REACTIONS reported from non recommended routes of administration).


Packages
DEPO-MEDROL Sterile aqueous suspension 40 mg per ml is available In the following presentations
(not all presentations may be marketed):
1 ml vial

5 ml vial


Properties
DEPO-MEDROL is a sterile aqueous suspension of the synthetic glucocorticoid methylprednisolone acetate. It has a strong and prolonged anti-inflammatory, immunosuppressive and anti-allergic activity. DEPO-MEDROL can be administered I.M. for a prolonged systemic activity as well as in situ for a local treatment. The prolonged activity of DEPO-MEDROL is explained by the slow release of the active substance.


PHARMACODYNAMICS
Methylprednisolone acetate has the general properties of the glucocorticoid methylprednisolone but is less soluble and less readily metabolised, which explains its prolonged activity.


Glucocorticoids diffuse across cell membranes and complex with specific cytoplasmic receptors. These complexes then enter the cell nucleus, bind to DNA (chromatin), and stimulate transcription of mRNA and subsequent protein synthesis of various enzymes thought to be ultimately responsible for the numerous effects after systemic use. Glucocorticoids not only have an important influence on inflammatory and immune processes, but also affect the carbohydrate, protein and fat metabolism. They also act on the cardiovascular system, the skeletal muscles and the central nervous system.


- Effect on the inflammatory and immune process:
The anti-inflammatory, immunosuppressive and anti-allergic properties of glucocorticoids are responsible for most of the therapeutic applications.


These properties lead to the following results:
- reduction of the immunoactive cells near the inflammation focus;
- reduced vasodilation;
- stabilization of the lysosomal membranes;
- inhibition of phagocytosis;
- reduced production of prostaglandins and related substances.


A dose of 4.4 mg methylprednisolone acetate (4 mg methylprednisolone) has the same glucocorticosteroid (anti-inflammatory) effect as 20 mg hydrocortisone. Methylprednisolone has only a minimal mineralocorticoid effect (200 mg methylprednisolone are equivalent to 1 mg desoxycorticosterone).


- Effect on carbohydrate and protein metabolism:
Glucocorticoids have a protein catabolic action. The liberated amino acids are converted into glucose and glycogen in the liver by means of the gluconeogenesis process. Glucose absorption in peripheral tissues decreases, which can lead to hyperglycemia and glucosuremia, especially in patients who are prone to diabetes.


- Effect on fat metabolism:
Glucocorticoids have a lipolytic action. This lipolytic activity mainly affects the limbs. They also have a lipogenetic effect which is most evident on chest, neck and head. All this leads to a redistribution of the fat deposits.


Maximum pharmacologic activity of glucocorticoids lays behind peak blood levels, suggesting that most effects of the drugs result from modification of enzyme activity rather than from direct actions by the drug.


PHARMACOKINETICS
Methylprednisolone acetate is hydrolised to its active form by serum cholinesterases. In man, methylprednisolone forms a weak dissociable bond with albumin and transcortin. Approximately 40 to 90% of the drug is bound. The intracellular activity of glucocorticoids results in a clear difference between plasma half-life and pharmacological half-life. Pharmacological activity persists after measurable plasma levels have disappeared.


The duration of anti-inflammatory activity of glucocorticoids approximately equals the duration of hypothalamic-pituitary-adrenal (HPA) axis suppression.


I.M. injections of 40 mg/ml give after approximately 7.3 1 hour (Tmax) methylprednisolone serum peaks of 1.48 0.86 g/100 ml (Cmax). The half-life is in this case 69.3 hours. After a single I.M. injection of 40 to 80 mg methylprednisolone acetate, duration of HPA axis suppression ranged from 4 to 8 days.


An intra-articular injection of 40 mg in both knees (total dose: 80 mg) gives after 4 to 8 hours methylprednisolone peaks of approximately 21.5 g/100 ml. After intra-articular administration methylprednisolone acetate diffuses from the joint into systemic circulation over approximately 7 days, as demonstrated by the duration of the HPA axis suppression and by the serum methylprednisolone values.


Metabolism of methylprednisolone occurs via hepatic routes qualitatively similar to that of cortisol. The major metabolites are 20 beta-hydroxymethyl-prednisolone and 20 beta-hydroxy-6 alpha-methylprednisone. The metabolites are mainly excreted in the urine as glucuronides, sulfates and unconjugated compounds. These conjugation reactions occur principally in the liver and to some extent in the kidney.

 

1    2    3    4    5

Abdomen
Blood
Bone
Breast
Ear

Eye

Face
Hair

Head

Heart
Kidney
Liver
Limbs
Lungs
newMind
Mouth
Muscles
Nails

Neck

newNerves
Nose

Skin

Teeth

Throat

Tongue
 
Health news
 
Cardiovascular Guide
 
Natural Remedies
 
Treatment of Cancer
 
Women's Health
 
Irritable bowel syndrome
 
Common Childhood Illnesses
 
Prescribed Drugs
 
 

     
         
     

 

Disclaimer