Pehacort

Uses

Pehacort is a corticosteroid used to treat inflammation or immune-mediated reactions and to treat endocrine or neoplastic diseases.

Pehacort is indicated as an anti-inflammatory or immunosuppressive drug for allergic, dermatologic, gastrointestinal, hematologic, ophthalmologic, nervous system, renal, respiratory, rheumatologic, infectious, endocrine, or neoplastic conditions as well as in organ transplant.

Pehacort is also used to associated treatment for these conditions: Acne Vulgaris, Acute Gouty Arthritis, Acute Lymphoblastic Leukaemias (ALL), Aggressive Lymphoma, Allergic Bronchopulmonary Aspergillosis, Allergic Rhinitis (AR), Allergic corneal marginal ulcers, Alveolitis, Extrinsic Allergic, Ankylosing Spondylitis (AS), Anterior Segment Inflammation, Aspiration Pneumonitis, Asthma, Atopic Dermatitis (AD), Bell's Palsy, Berylliosis, Bullous dermatitis herpetiformis, Chorioretinitis, Chronic Obstructive Airways Disease Exacerbated, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Corneal Inflammation, Crohn's Disease (CD), Dermatitis exfoliative generalised, Dermatitis, Contact, Dermatomyositis, Disseminated tuberculosis, Drug hypersensitivity reaction, Edema of the cerebrum, Epicondylitis, Erythroblastopenia, Giant Cell Arteritis (GCA), Hepatitis, Autoimmune, Hypercalcemia of Malignancy, Idiopathic Thrombocytopenic Purpura, Iridocyclitis, Iritis, Leukemia, Acute, Leukemias, Loeffler's syndrome, Malignant Lymphomas, Metastatic Castration Resistant Prostate Cancer, Multiple sclerosis exacerbation, Mycosis Fungoides (MF), Ocular Inflammation, Ophthalmia, Sympathetic, Optic Neuritis, Pain caused by Herpes zoster, Pemphigus, Pericarditis, Pneumocystis Jirovecii Pneumonia, Polymyalgia Rheumatica, Primary adrenocortical insufficiency, Proteinuria, Psoriatic Arthritis, Pulmonary Fibrosis, Pure Red Cell Aplasia, Relapsing Polychondritis, Rheumatic heart disease, unspecified, Rheumatoid Arthritis, Rheumatoid Arthritis, Juvenile, Seasonal Allergic Conjunctivitis, Secondary adrenocortical insufficiency, Secondary thrombocytopenia, Serum Sickness, Severe Seborrheic Dermatitis, Sjögren's Syndrome, Stevens-Johnson Syndrome, Systemic Lupus Erythematosus (SLE), Takayasu's Disease, Thyroid Eye Disease, Thyroiditis, Thyrotoxicosis, Trichinosis, Tuberculous Meningitis, Ulcerative Colitis, Uveitis, Vasculitis, Acquired immune hemolytic anemia, Acute Bursitis, Acute Tenosynovitis, Bronchiolitis obliterans organizing pneumonia, Fulminating Tuberculosis, Idiopathic eosinophilic pneumonias, Non-suppurative Thyroiditis, Severe Psoriasis, Solid organ rejection, Subacute Bursitis, Symptomatic Sarcoidosis, Synovitis of osteoarthritis, Systemic Dermatomyositis, Varicella-zoster virus acute retinal necrosis

How Pehacort works

Pehacort is first metabolized in the liver to its active form, prednisolone, a glucocorticoid agonist corticosteroid.

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation. Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive. High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.

Toxicity

Data regarding acute overdoses of prednisone are rare but prolonged high doses of prednisone can lead to a higher incidence and severity of adverse effects such as mental symptoms, moon face, abnormal fat deposits, fluid retention, excessive appetite, weight gain, hypertrichosis, acne, striae, ecchymosis, increased sweating, pigmentation, dry scaly skin, thinning scalp hair, increased blood pressure, tachycardia, thrombophlebitis, decreased resistance to infection, negative nitrogen balance with delayed bone and wound healing, headache, weakness, menstrual disorders, accentuated menopausal symptoms, neuropathy, fractures, osteoporosis, peptic ulcer, decreased glucose tolerance, hypokalemia, and adrenal insufficiency.

Food Interaction

• Avoid alcohol.
• Take with food. Food reduces irritation.

Pehacort Cholesterol interaction

[Moderate] Corticosteroids may elevate serum triglyceride and LDL cholesterol levels if used for longer than brief periods.

Patients with preexisting hyperlipidemia may require closer monitoring during prolonged corticosteroid therapy, and adjustments made accordingly in their lipid-lowering regimen.

Pehacort Hypertension interaction

[Moderate] Corticosteroids may cause hypernatremia, hypokalemia, fluid retention, and elevation in blood pressure.

These mineralocorticoid effects are most significant with fludrocortisone, followed by hydrocortisone and cortisone, then by prednisone and prednisolone.

The remaining corticosteroids, betamethasone, dexamethasone, methylprednisolone, and triamcinolone, have little mineralocorticoid activities.

However, large doses of any corticosteroid can demonstrate these effects, particularly if given for longer than brief periods.

Therapy with corticosteroids should be administered cautiously in patients with preexisting fluid retention, hypertension, congestive heart failure, and

Dietary sodium restriction and potassium supplementation may be advisable.

Pehacort Drug Interaction

Moderate: aspirin, furosemideMinor: fluticasone / salmeterol, albuterol, budesonide / formoterol, alprazolamUnknown: diphenhydramine, duloxetine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, esomeprazole, hydroxychloroquine, montelukast, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine

Pehacort Disease Interaction

Major: GI perforation, infections, PUD, vaccinationModerate: (+) tuberculin test, cirrhosis, depression/psychoses, diabetes, electrolyte imbalance, fluid retention, hyperadrenocorticalism, hyperlipidemia, hypothyroidism, liver disease, MI, myasthenia gravis, myopathy, ocular herpes simplex, ocular toxicities, osteoporosis, scleroderma, strongyloidiasis, thromboembolism

Volume of Distribution

Data regarding the volume of distribution for prednisone is not readily available. However, a 0.15mg/kg dose of prednisolone has a volume of distribution of 29.3L, while a 0.30mg/kg dose has a volume of distribution of 44.2L.

Elimination Route

Oral prednisone has a T_max of 2 hours, while the delayed-release formulation has a T_max of 6-6.5 hours. A 5mg dose of prednisone has an AUC of 572mL/min/1.73m^{2 Data regarding the C_max of prednisone is not readily available.}

Half Life

Pehacort and its active metabolite prednisolone have half lives of 2-3 hours from both immediate and delayed release preparations.

Clearance

Data regarding the clearance of prednisone is not readily available.

A 5.5µg/h/kg infusion of prednisolone has an average clearance of 0.066±0.12L/h/kg, while a 0.15±0.03L/h/kg infusion has an average clearance of 0.15L/h/kg.

Elimination Route

Pehacort is excreted mainly in the urine as sulfate and glucuronide conjugates.

Innovators Monograph

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