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  1. Tranexamic Acid
    Anti-fibrinolytic agent

    INT: treatment of clyclic heavy menstrual bleeding

    Ovulation and Gonadotropin Stimulants
  2. Clomiphene Citrate
    • Treatment of ovarian failure and male infertility
    • Increase pituitary output of gonadotropins
  3. Chorionic gonadotropin
    • INT: prepubertal cryptorchidism, hypogonadism,
    • ovulation stimulation
  4. Chorionic gonadotropin alpha
    INT: final follicular maturation, ovulation induction
  5. Gonadorelin Acetate
    Polypeptide with chorionic gonadotropin activity

    INT: primary hypothalamic amenorrhea
  6. Nafarelin acetate
    Polypeptide with chorionic gonadotropin activity

    • INT: precocious puberty (early puberty) and
    • endometriosis
  7. Histrelin Acetate
    Polypeptide with chorionic gonadotropin activity

    INT: central precocious puberty
  8. Lutropin Alfa
    • Recombinant form of human luteinizing hormone from
    • hampsters

    • INT: Stimulation of follicular development in
    • hypogonadotropic hypogonal women with luteinizing hormone deficiency
  9. Abarelix
    • INT: treatment of advanced prostate cancer to
    • achieve medical castration

    • MOA: direct and competitive inhibitor of
    • gonadotropin releasing hormone receptors in pituitary

    Only doctors with PLUS program may prescribe
  10. Androgen and anabolic steroids
    Small quantities in females

    Primary sex hormones of males 2 types of activity

    • Androgenic activity – male sex characteristic
    • promotion

    Anabolic activity – muscle building activity

    • Two natural hormones – testosterone and
    • 5alpha-dihydrotestosterone
  11. Therapeutic uses of androgen and anabolic agents
    Androgen replacement therapy in men

    • Testosterone deficiency through hypogonadism or
    • hypopituitarism

    Low doses in women to treat postpartum breast enlargement

    • Selected use in women for advanced or metastatic carcinoma
    • of the breast

    • Used to treat certain anemias, osteoporosis, and
    • stimulate growth in post-puberty boys

    • Anabolics contraindicated in men with family
    • history of prostate or testicular cancer

    • DI: incrase anticoagulant activity, interference
    • with lab tests
  12. Testosterone
    Short acting testosterone product

    INT: Hypogonadism
  13. Testosterone Enanthate and Testosterone Cypionate
    Long acting testosterone products

  14. Methyl Testosterone


    • INT: endometriosis, fibrocystic breast disease,
    • hereditary angioedema

    MOA: inhibits pituitary gonadotropins
  15. Finasteride
    • INT: begign prostatic hyperplasia, androgenic
    • alopecia

    • MOA: Inhibits conversion of testosterone to
    • 5alpha-dihydrotestosterone via 5alpha-reductase inhibition
  16. Dutasteride
    INT: benign prostatic hyperplasia

    • MOA: Inhibits conversion of testosterone to
    • 5alpha-dihydrotestosterone via 5alpha-reductase inhibition
  17. Alfuzosin HCl

    INT: Benign prostatic hyperplasia

    • MOA: selective blockade of smooth muscle
    • post-synaptic alpha1-adronergic receptors

    50% reduction in absorption w/o food

    Extensively metabolized by CYP3A4
  18. Silodosin

    INT: benign prostatic hyperplasia

    • MOA: selective blockade/antagonism of smooth
    • muscle post-synaptic alpha1a-adrenergic receptors

    Take with food
  19. Oxandrolone
    Steroids used for anabolic activity

    • INT: adjuctive to promote weight gain after
    • surgery, chronic infections, severe trauma, HIV wasting syndrome
  20. Oxymetholone
    Steroids used for anabolic activity

    INT: Anemias
  21. Oxandrolone decanoate
    Steroids used for anabolic activity

    INT: anemias of renal insufficiency
  22. Stanoxzolol
    INT: hereditary angioedema
  23. Ecallantide
    Human plasma kallkrein inhibitor


    INT: acute attacks of hereditary angioedema

    MOA: Directly inhibiting kallikrein

    Watch for anaphylaxis
  24. Icatibant
    INT: acute attacks of hereditary angioedema

    MOA: selective bradykinin B2 receptor antagonist
  25. Lenalidomide
    Nonsteroidal used for anemia

    • INT: transfusion-dependent anemia due to low or
    • intermediate risk myelodysplastic syndrome (MDS)


    • Adverse effects: neutropenia, thrombocytopenia,
    • increased risk of blood clots and pulmonary emboli

    Uterine-active agents
  26. Mifeprisotone

    • BLACK BOX: may cause life threatening infection
    • due to incomplete abortion

    MOA: Progesterone antagonist

    New indication for Cushing’s Disease

    • MOA: antagonist of one of the body’s two cortisol
    • receptors and progesterone receptors

    • Useful in treating psychosis and depression
    • associated with Cushing’s
  27. Dinoprostone and Carboprost Tromethamine

    • MOA: stimulates uterine contractions, used in
    • conjuction with surgical methods such as saline-injections or suction abortion
  28. Dinoprostone
    INT: labor induction in conjuction with oxytocin

    MOA: stimulates uterine contractions
  29. Oxytocin
    INT: induction of labor via IV drip

    • MOA: natural pituitary hormone that increases
    • uterine contractions
  30. Ergonovine Maleate
    Post-partum or postabortal bleeding

    • MOA: partial antagonist/agonist of
    • alpha-adrenergic, dopaminergic or tryptaminergic receptor of uterine tissue
    • increasing uterine contractions and decreasing bleeding
  31. Methylergonovine maleate
    Post-partum or post-abortal bleeding
  32. Ritodrine
    INT: management of pre-term labor

    • MOA: a beta2-receptor agonist that decreases
    • uterine smooth muscle contractions
  33. Biphosphonates
    • Slow the formation and dissolution of
    • hydroxyapatite crystals

    • MOA: bisphosphonate is incorporated into the bone
    • matrix and is imbibed by osteoclasts. This incapacitates the osteoclast
    • preventing resorption of the bone

    • INT: paget’s disease, malignancy induced
    • hypercalcemia, postmenopausal osteoporosis, metastatic cancer of the bone,
    • ossification caused by injury or total hip replacement

    • Use caution in renal impairment, avoid Al and Mg
    • containing antacids, may cause nausea and diarrhea
  34. Biphosphonate Products



    Tiludronate sodium

    Risendronate Sodium
  35. Zoledronic acid
    New Biphosphonate product

    • INT: hypercalcemia due to malignancy, IV once
    • yearly for osteoporosis and paget’s
    • disease
  36. Ibondronate sodium
    New bisphosphonate product

    Indicated postmenopausal osteoporosis
  37. Teriparatide
    • INT: treatment of osteoporosis in both men and
    • women at increased risk of fracture

    • MOA: a recombinant human parathyroid hormone,
    • unique in that it actually stimulates new bone formation

    Increased risk of osteosarcoma

    SubQ injection
  38. Denosumab
    • INT: treatment of postmenopausal women with
    • osteoporosis at high risk of fracture

    MOA: RANK ligand inhibitor

    Injection given once every six months
  39. Cinalcalcet HCl
    New calcimimetic

    • INT: treatment of secondary hyperparathyroidism
    • dialysis patients with chronic kidney disease, hypercalcemia secondary to
    • parathyroid carcinoma

    • MOA: increases the sensitivity of the Ca+2
    • sensing receptor on parathyroid gland chief cells that regulate the production
    • of PTH
  40. Adrenocortical Steroids
    Major mineralcorticoid is aldosterone

    Major glucocorticoid is cortisol

    Release regulated by ACTH secretions by the pituitary
  41. Addison’s Disease
    • Primary adrenocortical insufficiency – requires replacement
    • therapy of both glucocorticoids and mineralcorticoids

    • Secondary adrenocortical insufficiency – Due to
    • inadequate ACTH secretion
  42. Cushing’s Disease
    • Caused by excessive secretion of glucocorticoids as
    • a result of excessive ACTH secretions or a primary adrenal source such as a
    • tumor

    • Best treatment is surgical but adrenal steroid
    • inhibitors can be used
  43. Iatrogenic Cushing’s
    Caused by prolonged treatment with glucocorticoids

    • Common symptoms: euphoria, buffalo hump, thinning
    • of the skin, increased abdominal fat, Thin arms and legs with muscle wasting,
    • increased bruising and poor wound healing, moon face w/ read cheeks

    Increased susceptibility to infection
  44. Aminogluethimide
    • Adrenal steroid inhibitor (prevents the conversion
    • of cholesterol to pregnenolone)

    • INT: Cushing’s syndrome, postmenopausal patients
    • with advanced breast and prostate carcinoma
  45. Corticotropin
    ACTH injection and a repository product

    • INT: diagnostic testing of adrenal function ,
    • nonsupprurative thyroiditis, hypercalcemia associated with cancer, acute
    • multiple sclerosis
  46. Cortone Acetate
    Glucocorticoid product
  47. Fludrocortisone Acetate
    Mineralcorticoid product

    • INT: primary or secondary adrenal insufficiency,
    • management of severe orthostatic hypotension
  48. Leflunomide
    INT: rheumatoid arthritis

    MOA: inhibitor of de novo pyrimidine synthesis

    • Contraindications: pregnancy or desire to get
    • pregnant

  49. Sometrem and Somatropin
    Can be used to treat growth failure
  50. Mesasermin
    Recombinant insulin-like growth factor 1

    • INT: treatment of growth failure in children with
    • severe primary insulin-like growth factor
  51. Octreotide Acetate
    INT: acromegaly, tumors, GI fistula, diarrheal states, hypoglycemia due to excess insulin
  52. Somatuline
    INT: long-term treatment of acromegalic patients who have had an inadequate response to or cannot be treated with surgery or radiotherapy
  53. Nitisinone
    Orphan Drug

    Treatment of hereditary tyrosinemia type 1

    • Caution: results in elevated plasma levels of
    • tyrosine so must watch diet
  54. Calcitonin-Salmon
    Isolated from salmon

    • INT: used in postmenopausal osteoporosis, paget’s
    • disease, hypercalcemia

    • MOA: Calcitonin suppresses resorption of bone by
    • inhibiting the ctivity of osteoclasts

    Must be coadministered with Calcium
  55. Conivaptan HCl
    INT: euvolemic hyponatremia – too little Na present in the blood stream but normal amount of fluid

    MOA: non-peptide, dual antagonist of arginine vasopressin receptors
  56. Tolvaptan
    INT: hypervolemic and euvolemic hyponatremia patients with HF, cirrhosis and inappropriate antidiuretic hormone secretion

    MOA: oral selective vasopressin-receptor antagonist

    Metabolized by CYP3A
Card Set:
2012-04-25 20:19:04
MEDCHEM UWYO Quiz 10 Drugs

All Drugs for Final MEDCHEM 1 quiz
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