Liothyronine sodium (Cytomel)

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Name: Liothyronine sodium (Cytomel)

Class: Thyroid Hormone

Mechanism: Sodium salt of T3. T3/T4 synergize w/GH effects, increase BMR, potentiate catecholamine effects on heart, promote lipolysis, and decrease serum cholesterol.

Absorption: Oral ® 95% absorption.

Dist.: Poor placental transfer ® okay for pregnant E. Little in milk (use cautiously).

Metabolism.: Hepatic conjug. w/glucuronic & sulfuric acids.

Excretion, : Bile; some lost in stool due to enterohepatic circ. £ 2 d.

Toxicity/S.E.s: Salicylates and dicumarol compete for albumin binding sites ® marked increase of free levels.

Utility: Preferred in treatment of myxedema coma. Treat hypothyroidism and goiter (not due to iodine deficiency or hyperthyroidism).

Special Features: 50-75 mg/d. 4x the potency of levothyroxine sodium, but same efficacy.

 

Levothyroxine sodium (Synthroid, Levothroid, Levoxine)

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Name: Levothyroxine sodium (Synthroid, Levothroid, Levoxine)

Class: Thyroid Hormone

Mechanism: Sodium salt of T4. T3/T4 synergize w/GH effects, increase BMR, potentiate catecholamine effects on heart, promote lipolysis, and decrease serum cholesterol.

Absorption: Incomplete oral absorption—30-40% recovered in stool.

Dist.: Poor placental transfer ® okay for pregnant E. Little in milk (use cautiously).

Metabolism.: Hepatic conjug. w/glucuronic & sulfuric acids. Peripheral deiodination to T3.

Excretion, : Bile; some lost in stool due to enterohepatic circ. 6-7 d.

Toxicity/S.E.s: Salicylates and dicumarol compete for albumin binding sites ® marked increase of free levels.

Utility: Treat hypothyroidism and goiter (not due to iodine deficiency or hyperthyroidism).

Special Features: 200-300 mg/d. 1/4 the potency of liothyronine sodium, but same efficacy.

 

Thyroglobulin (Proloid)

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Name: Thyroglobulin (Proloid)

Class: Thyroid Hormone

Mechanism: T3/T4 synergize w/GH effects, increase BMR, potentiate catecholamine effects on heart, promote lipolysis, and decrease serum cholesterol.

Absorption: Oral

Dist.: Poor placental transfer ® okay for pregnant E. Little in milk (use cautiously).

Metabolism.: T4 & T3 released by proteolysis after ingestion. Hepatic conjug. of T4/T3 w/glucuronic & sulfuric acids.

Excretion, : Bile; some lost in stool due to enterohepatic circulation.

Toxicity/S.E.s: Salicylates and dicumarol compete for albumin binding sites ® marked increase of free levels.

Utility: Treat hypothyroidism and goiter (not due to iodine deficiency or hyperthyroidism).

Special Features: 120-180 mg/d. Similar efficacy to levothyroxine sodium and liothyronine sodium, although dose not standardized by bioassay

 

Misoprostol (Cytotec)

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Name: Misoprostol (Cytotec)

Class: Gastric Protectant (Prostaglandin)

Mechanism: Analog of prostaglandin E1. Inhib. secretion of HCl. Stimulates secretion of mucus & HCO3 (cytoprotective).

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Toxicity/S.E.s: Diarrhea, nausea. Produces uterine contractions. \ c/i during pregnancy.

Utility: Only agent approved for prevention of gastric ulcers induced by NSAIDs. Less effective than H2 antagonists for acute treatment of peptic ulcers.

Special Features:

 

Bacillus Calumet-Guerin (BCG)

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Name: Bacillus Calumet-Guerin (BCG)

Class: Immunostimulant

Mechanism: Viable strain of Mycobaterium bovis. Enhances Mf activity, promotes Mf tumoricidal activity.

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Utility: Treat bladder carcinoma and melanomas.

Special Features:

 

Interferon g

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Name: Interferon g

Class: Immunostimulant

Mechanism: Binds to cell-surface receptors ® activation of NK cells and Mfs, promotion of conversion to TH1 cells.

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Toxicity/S.E.s: Fever w/chills; dose-related leukopenia, thrombocytopenia; fatigue, malaise, anorexia, weight loss, alopecia, transient elevation of liver enzymes. High doses may ® transient & reversible nephrotoxicity.

Utility: Used to treat for chronic hepatitis B, virally induced tumors, recurrent varicella zoster, HSV keratitis, Kaposi’s sarcoma, hairy cell leukemia, cutaneous T cell lymphoma.

Special Features: Produced by memory TH1 cells and NK cells. Interferon production is induced by dsRNA (poly I:C), ampligen (mismatched nucleotides), LPS.

 

Interferon b

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Name: Interferon b

Class: Immunostimulant

Mechanism: Binds to cell-surface receptors ® inhib. of viral replication, inhib. of cell proliferation.

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Toxicity/S.E.s: Fever w/chills; dose-related leukopenia, thrombocytopenia; fatigue, malaise, anorexia, weight loss, alopecia, transient elevation of liver enzymes. High doses may ® transient & reversible nephrotoxicity.

Utility: Used to treat for chronic hepatitis B, virally induced tumors, recurrent varicella zoster, HSV keratitis, Kaposi’s sarcoma, hairy cell leukemia, cutaneous T cell lymphoma.

Special Features: Produced by fibroblasts. Interferon production is induced by dsRNA (poly I:C), ampligen (mismatched nucleotides), LPS.

 

Interferon a

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Name: Interferon a

Class: Immunostimulant

Mechanism: Binds to cell-surface receptors ® inhib. of viral replication, inhib. of cell proliferation.

Absorption:

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Toxicity/S.E.s: Fever w/chills; dose-related leukopenia, thrombocytopenia; fatigue, malaise, anorexia, weight loss, alopecia, transient elevation of liver enzymes. High doses may ® transient & reversible nephrotoxicity.

Utility: IFN a2A is approved for mgt. of hairy cell leukemia. Also useful for chronic hepatitis B, virally induced tumors, recurrent varicella zoster, HSV keratitis, Kaposi’s sarcoma, cutaneous T cell lymphoma.

Special Features: Produced by mononuclear leukocytes. Interferon production is induced by dsRNA (poly I:C), ampligen (mismatched nucleotides), LPS.

 

Erythropoietin (Epoetin Alfa, Epogen)

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Name: Erythropoietin (Epoetin Alfa, Epogen)

Class: Immunostimulant

Mechanism: Stim. division/differentiation of erythroid progenitors in bone marrow.

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Toxicity/S.E.s: Usu. well-tolerated. Low incidence of hypertension, headache, seizures. Rare hypersensitivity rxns.

Utility: Treat anemia assoc. w/chronic renal failure, AZT therapy, cancer and chemotherapy. Supplemental iron eventually required in therapy.

Special Features: Manufactured by recombinant DNA technology. Identical to human erythropoietin.

 

GM-CSF (Sargramostim)

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Name: GM-CSF (Sargramostim)

Class: Immunostimulant

Mechanism: Stim. bone marrow production of precursors to PMNs, monocytes, platelets. Also activates PMNs, eosinophils, and monocytes.

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Toxicity/S.E.s: Fever, dermatologic rxns, splenomegaly.

Utility: FDA-approved to increase myeloid recovery rate after bone marrow transplantation. Also used for hematological reconstitution after autologous bone marrow transplants and treatments w/bone marrow cytotoxic drugs.

Special Features: Greater severity of immunologic S.E.s than w/G-CSF.