Steroids Part II MedChem Quiz

• Tranexamic acid
• Indications: treatment of cyclic heavy menstrual bleeding
• MOA: a synthetic lysine aa derivative which diminishes the dissolution of hemostatic fibrin plasmin the lysine receptor binding sites of plasmin are occupied, preventing preventing binding to fibrin monomers, thus preserving and stabilizing fibrin's matrix structure

• Indications: treatment of ovarian failure and male onfertility
• MOA: appears to increase pituitary output of gonadotropins

INdications: prepubertal cryptochidism, hypogonadism ovulation stimulations

• Chorionic gonadotropin alpha
• INdication final follicular maturation ovulation induction

• Gonadorelin acetate
• Primary hypothalmic amenorrhea

• Nafarelin acetate
• Endometriosis and central precocious puberty

• Histrelin
• Central precocious puberty
• Vantus implant palliative treatment of advanced protstate cancer by decreasing testosterone levels to castrate concentrations following the first week of use

• Urofollitropin --Ferinex polycystic ovary syndrome follicular stimulation
• Follitropin alpha --Gonal ovulation induction follicule stimulation
• Follitropin beta -- Follistim ovulation follicle stimmulation
• Menotropins

• Lutropin alfa for injection
• Indications: stimulation of folliculuan development in infertile hypogonadotropic hypogonal women with profound luteininzing hormone deficiency

• Abarelix
• Indication: treatment of adavance prostate cancer to ahieve medical castration, for those that will not undergo surgical castration or hormonal treatment sever bone pain from metastatic disease
• MOA: a direct and cometitive blocker of gonadotropin releasing hormone receptors in the pituitary gland--- directly suppresses luteinizing and follicle stimulating hormone secretion reducing the secretion of testosterone by the testes
• Synthetic decapeptide

• A metabolite of testosterone from 5 alpha reductase activity necessary for maintaining proper prostate function in men
• 17 ketone is inactive

• Therapeutic use:n replacement therapy
• Low doses can be used in women to treat dymenorrhea and postpartum breast enalargement and lack of libido
• Selected use in women in advanced or metastatic carcinoma of the breast

Testosterone long acting products in oil base for injection

• Tesamone aqueous suspension
• SC pellets Testopel
• Transdermal Testoderm ANdroderm
• Striant buccal mucoadhesive adheres to the gum tissue above the incisiors
• topical solution for hpoygonadism Axiron FOresta

Testosterone long acting produts in oil base for injection prodrug

Oreton Methyl Tablets

fluoxymestrone tablets

• Finasteride
• Indications: Benign prostatic hyperplasia androgenic alopeica
• MOA: inhibit steroid 5 alpha reductase preventing conversion to 5 alpha dihydroxytestosterone

• Dutasteride
• MOA: inhibits steroid 5 alpha reductast preventing testosterone conversion to 5 alpha dihydroxytestosterone
• INdications: benign prostatic hyperplasia

• Alfuzosin
• Indications: benign prostatic hyperplasia
• MOA: selective blockage of smoothe muscle post synaptic alpha 1 receptors in the bladder neck and prstate that results in relaxation that improve urine flow and reduces symptoms

• Indications: benign prostatic hyperplasia
• MOA: selective blockage/antagonism of smoth muscl post synaptic alpha 1A adrenergic receptors in the bldder neck and postate that results in relaxation that improves urine flow and reduces symptoms

• Oxandrolone
• USed for anabolic activity
• INdications: adjuctive to promote weight gain after surgery chronic infection severe traum HIV wasting syndrome

• Oxyemthonlone
• Used for anabolic activity
• Indication anemias

• Oxandrolone decanoate
• O Indication: anemias of renal insufficiency
• USed for anabolic acitivity

• Stanoxzolol
• Hereitary angioedma
• Dnanzol

• C-- for prophylaxis
• B-- for acute attacks
• Proterin product derived from human plasma C1 esterase inhibitors
• Regulates clotting and inflammatory reactions that lead to local tissue swelling

• Ecallantide
• A human plasma kallkrein inhibitor
• INdications: acute attacks of hereditary angioedema
• MOA: Ecallantide exerts its effect by directly inhibiting kallikrein therby reducing decessing bradykinin production and symptoms of localized swelling inflammation and pain
• watch for anaphylaxis

• Icatibant
• Indication: acute attacks of hereditary angioedema
• MOA: selective bradykinin B2 receptor antagonist which prevents incontrollable vascular permeability and angioedema

• Lenalidomide
• Indications: Tranfusion dependent anemia due o low or intermediate -1 risk myelodyplastic syndrome, MDS is where bone marrow does not produce enoguh mature blood cells
• MOA: Largely unknown immunodulator and antiangiogenic properties inhibit secretion of pro inflammatory cytokines increase the scretio of anti-flammatory cytokines from perpheral blood monouclear cells inhibits COX2 but not COX1
• Cause flipper babies

• MIfepristone RU-486
• Progesterone antagonist binds both progesterone and glucocorticoid receptor competitively no estrogenic activity

MOA: stimulates uterine contractions used in conjuction with srugical methods such as saline injeciton or suction abortion

• Prostaglandin E2 Prostin E2
• Agents for cervical ripeing or labor induction
• INdcaitions used to induce labor in conjuction with xytocin
• MOA stimualtes uterine contractions

• Oxytocin
• Indication : induction of labor via IV drip
• MOA natural pituitary hormone that increases uterine contractions

• Ergonovine maleate
• MOA: Partial antagonist/agonist of alpha adrenergic dopaminergic or trypaminergic recpeto of uterine tissue increasing uterine contractions and decresing bleeding

• Methylergonovine maleate
• MOA: Partial antagonist/agonist of alpha adrenergic dopaminergic or trypaminergic recpeto of uterine tissue increasing uterine contractions and decresing bleeding

• Ritodrine
• INdication: management of pre term labor
• MOA:: Beta receptor agonist that decreases uterine smooth muscle contraction

• Appears the bisphosphonate is incorporated into the bone matrix and is imbibed by osteoclast. this incapcitates the osteoclast preventing resorption of the bone
• Indications: Paget's disease

• Didronel-- Etidronate
• Aredia -- Pamidronate
• Fosamax --Alendronate
• Tiludronate -- Skelid
• Actonel -- Risedornate-- monthly dosing

• Zoledronic ACid
• New generation of bisphosphonate
• Hypercalcemia due to malignancy

• Zoledronic acid
• IV administration once yearly for osterporosis, Paget's Disease
• Claims to have a better reposnse rate measured as a drop in serum calcium levels when comapred to other bisphosphonate

• Ibandronate
• New generation of bisphosphonate
• Indicated postmenopausal osteoporosis
• Renal clearance is linearly related to creatinine clearance

Yes bisphosphonates have been shown to inhibit farnesyl transferase an enzyme involved in the Ras oncogene pathway

• Teriparatide
• Indications: treatment of osteoporosis in both men and women at increased risk of fracture
• MOA: A recombinant human parathyroid hormone containing 34 aa of the natural 84 aa humam parathyroid hormone

• Denosumab
• Indication: Treatment of postmenopausal women with osterporosis at high risk for fracture
• MOA: RANK ligand inhibitor. Rank is a transmembrane or soluble protein essential for the formation function and survival of osteoclasts. Prolia prevents RANKL from acitivating its receptor -- prevention of the RANKL/RANK interaction inhibits osteoclast formation function and survival therby decreasing bone resorption and increasing bone mass

• Denosumab
• Preventon of skeletal related events such as pathological fracture spinal cord compression or radiation to the bone in patients with bone metastases from solid tumors

Produced in the adrenal cortex of the body is aldosterone (controlled by K+ and renin-aldosterone system and results in enzyme synthesis reponsible for acitve ion transport)

• Cortisol
• Physiological regulation of synthesis and release is controlled by corticotropin (ACTH) which is secreted by the anterior pituitary gland
• Low plasm cortisol levels lead to increasaed secretion of ACTH
• High plasma levels leads to decreased secretion of ACTH
• ACTH secretion can be stimulated by emtional, physical or chemical stress and is controlled in a diurnal circadian pattern

• Aminogluethimide
• Indication: cushing syndrome postmenopausal patients with advanced breast and prostate carcinoma
• Prrevents the conversion of cholesterol to pregnenolone

• Mifepristone RU-486
• MOA: antagonist of one of the body's two cortisol receptors and progesterone receptor
• Useful in treating psychosis and depression associated with cushings

• INdications: Diagnostic test of adrenal function
• Nonsuppurative thyroiditis
• Hypercalcemia associated with cancer
• ACute multiple sclerosis

• Cortisone
• Indications: Primary and secondary adrenal insufficiency
• Collagen disease
• Dermatologic diseases
• Allergic states
• Ophthalmic inflammation
• Respiratory diseases
• Hematologic disorders
• Neoplastic disease such as leukemias
• Edematous states
• GI disease
• Acute mountain sickness