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LORACORT L.A. R Betamethasone L.A. of physiologic doses or low pharmacologic doses is not considered likely to For most indications glucocorticoid administration provides symptomatic Children
relief but has no effect on the underlying disease processes. Use of these Because infection such as chickenpox or measles may be more serious (or medications does not eliminate the need for other theraphies that may be even fatal) in children receiving immunosuppressant doses of corticosteroids,extra care to avoid exposure to these infections is recommended.
Usual adult and adolescent dose
Chronic use of corticosteroids may suppress growth and development of the Intra-articular. 1.5 to 12 mg, depending upon the size of the affected joint, pediatric and should be undertaken with caution.
Pregnant women
Intrabursal. 6mg, repeated as needed.
Corticosteroids cross the placenta. Although adequate studies have not been Intradermal or intralesional. 1.2 mg per square centimeter of affected skin done in humans, there is some evidence that pharmacologic doses of up to a total amont of 6mg, repeated at one-week intervals, if necessary.
corticosteroids may increase the risk of placental insufficiency, decreased Intramuscular. 500 mcg (0.5 mg) to 9 mg a day.
birthweight, or stillbirth. However, teratogenic effects in humans have not Usual pediatric dose
Dosage has not been established for Loracort L.A.
The elderly
For Loracort; in adrenocortical insufficiency-IM, 17.5 mcg (0.0175mg) (base) Geriatric patients may be more likely to develop hypertension during per kg of body weight a day(in 3 divided doses) every third day, or 5.8-8.75 mcg (0.0058-0.00875 mg) (base) per kg of body weight once a day is 10- Drug interactions
Potentially hazardous interactions
Contraindications
Barbiturates, hydantoins and rifampin.They may decrease pharmacologic Except under special cricumstances,these medications should not be used when the following medical problems exist: Oral contraceptives,estrogens and ketoconazole. They may decrease 1- In the case of intra-articular injection; prior arthroplasty of joint, blood clotting disorders, current or history of periarticular infection, non-arthritic Potentially useful interactions
juxta-articular osteoporosis, and unstable joint are contraindications.
Cyclosporine. The combination of two drugs is therapeutically beneficial for 2- In the case of neonatal respiratory distress syndrome prophylaxis; amnionitis, uterine bleeding, febrile illness or infection, active herpes type II infection,
viral keratitis, placental insufficiency, and premature membrance rupture are
contraindications.
8- Adverse reactions
Potentially life-threatening effects
The use of corticosteroids can lead to produce diabetes, local or systemic
infection, psychic disturbances, seizures, hypertension, tachycardia,
musculoskeletal disorders, Cushing syndrome, endocrine imbalance,
hypokalemic syndrome and myopathy.
Symptomatic adverse effects
These effects are visual disturbances, local irritation, tissue atrophy,scavring
at injection site and edema.
Interference with clinical pathology tests
Urine glucose and serum cholesterol levels may increase.
9- High risk groups
Neonates
Prenatal administration of Loracort to the mother to prevent respiratory distress syndrome in the premature neonate has not been shown to affect thechild’s growth or development adversely.Physiologic relplacement doses of Betamethasone(as Disodium Phosphate)4 mg/1 ml corticosteriods administered for treatment of maternal adrenal insufficiency are also unlikely to adversely affect the fetus or neonate.
Breast milk. Problems in human have not been documented. Administration Betamethasone(as Disodium Phosphate)3 mg/1 ml studies show increased incidence of cleft palate, placental insufficiency,
spontaneous abortions, or intrauterine growth retardation.
4- Clinical pharmacology
Glucocorticoids stimulate protein catabolism and induce enzymes responsible
for metabolism of amino acids. They decrease synthesis and increase
degradation of protein in lymphoid tissue, connective tissue, muscle, and
skin. Glucocorticoids increase glucose availability by inducing hepatic
enzymes involved in gluconeogenesis. They increase lipolysis and mobilize
fatty acids from adipose tissues.
Glucocorticoids decrease bone formation and increase bone resorption. They
reduce plasma calcium concentration, leading to secondary hyperparathyro-
idism and subsequent stimulation of osteoclasts, and directly inhibit osteoblasts.
Systemic effects of corticosteroids may be seen, such as fluid retention,
hypertension, adrenal suppression, and peptic ulceration.
5- Pharmacokinetics
Absorption
In parenteral use (I.M) freely soluble ester (sodium phosphate) is rapidly
1-Chemistry
absorbed and poorly soluble derivative (acetate) is slowly but completely absorbed. In local use, freely soluble ester is less rapidly absorbed than with Betamethasone Disodium Phosphate- C22H28FNa2O8P intramuscular injection and poorly soluble derivative is slowly but completelyabsorbed. Biotransformation is primarily hepatic (rapid) and also renal and tissue; mostly to metabolites. Following intramuscular administration the duration of action depends upon the solubility of the dosage form as well as the biological (tissue) half-life. Following local injections the duration dependsupon the solubility of the dosage form and the specific route/site of administration.
6- Metabolism
As a general rule, the metabolism of steroid hormones involves sequential additions of oxygen or hydrogen atoms, followed by conjugation to formwater-soluble derivatives and occurs in the liver.
2- Pharmacology
7- Therapeutic use
Loracort is a glucocorticoid that, when given systemically has potent Mode of use
glucocorticoid activity and binds with high affinity to the glucocorticoid It is recommended that intra-articular injections be repeated no more often receptor. Loracort would thus have catabolic effects and antianabolic effects on proteins in peripheral utilization of glucose, and indice calcium loss from Following intra-articular injection,the injected joint should not be over used, bone. Loracort has both local anti-inflammatory and immunosuppressive even if pain is relieved. It is recommended that weight-bearing joints be activity. Thus Loracort inhibitis the adherence of neutrophils and monocyte rested for 24 to 48 hours postinjection.
macrophages to the capillary endothelial cells of the inflamed area. The drug Administration of a local anesthetic concurrently with intra-articular or soft blocks the effect of macrophage migration inhibitory factor and decreases tissue injection of Loracort L.A. may reduce the pain of injection and provide the activation of plasminogen to plasmin. Finally, by inhibition of phospholipase A2 activity, via formation of lipocortin, Loracort reduces the formation of Dosages for local injections (e.g., intra-articular, intrabursal, intradermal, prostaglandins and leukotrienes in local tissue.
intralesional) are given up to 9mg (base) as ranges only.
3- Toxicology
When Loracort L.A. is administered intramuscularly, it should be injected Cortisol causes a high incidence of cleft palate in some strains of mice. The deeply into the gluteal to prevent local tissue atrophy and it should be shaked position in humans is less clear. First-trimester exposure to cortisone has well. It is recommended that the deltoid muscle not be used because of a been reported in 35 cases and 9 of the infants had congenital malformations higher incidence of local atrophy. Loracort L.A. should not be used which included cleft lip, coarctation of the aorta, interventricular septal intravenously. Shake well it befor use.
defect, clubfoot, undescended testes, hydrocephatus, cataracts, and cyclopia.
Indications
Pharmacological doses in animals show some evidence of increased risk of 1- Replacement therapy (treatment of adrenal insufficiency states) placental insufficiency, decreased birthweight, or stillbirths; other animal 2- Symptomatic therapy (anti-inflammatory and immunosuppressant

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