Endocrine drugs Flashcards

1
Q

Drug that is purified from the urine of postmenopausal women and is used to promote spermatogenesis

A

Urofollitropin

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2
Q

A 3 year old boy with failure to thrive and metabolic disturbance was found to have an inactivating mutation in the gene that encodes the growth hormone receptor. Which drug will most likely improve his metabolic function and promote its growth

A

Mecasermin

  • a combiantion of recombinant IGF-1 and the binding protein that protects IGF-1 from immediate destruction
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3
Q

An important difference between leuprolide and ganirelix is that ganirelix _____

A

immediately reduces gonadotropin secretion

  • Leuprolide
    • agonist of GnRH receptors
    • about 1 week of sustained activity
  • Ganirelix
    • GnRH antagonist
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4
Q

used to treat the amenorrhea-galctorrhea syndrome

A

Bromocriptine

  • dopamine receptor agonist
    • drug should not be used in patients with a history of schizophrenia or other forms of psychotic illness
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5
Q

Patient is a known case of turner syndrome. Which drug will allow her to achive a higher adult height

A

Somatropin

  • recombinant human GH
    • Turner syndrome or chronic renal failure
  • ACTH
    • used in diagnosisng adrenal insuffciency
  • CRH
    • distringuish cushing’s syndrome from ectopic ACTH secretion
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6
Q

Most appropriate drug to treat precocius puberty

A

Leuprolide

  • GnRH agonist
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7
Q

Pharmacologic treatment for acromegaly

A

Octreotide

  • somatostatin analog. has some efficacy in reducing the excess GH production
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8
Q

The 2nd step in ovulation induction is the administration of a drug with FSH activity.

A

Follitropin

  • Recombinant FSH
  • hCG - LH analog
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9
Q

treatment for pituitary diabetes insipidus

A

Desmopressin

  • V2 receptor
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10
Q

Somatropin

A

Recombinant human GH. Actis through GH receptors to icnrease the production of IGF-1

Replacement in GH deficienct. Icnreased final adult height in children with certain conditions associated with short stature. Wasting in HIV infection. Short bowel syndrome

SQ injection

SE: In children, pseudotumor cerebri, slipped capital femoral epiphysis, progression of scoliosis, edema ,and hyperglycemia. In Adults, peripheral edema, myalgia,and arthralgias. Risk os asphyxia in severely obese patients with Prader Willi syndrome and upper airway obstruction or sleep apnea

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11
Q

Mecasermin

A

IGF-1 agonist

Replacement of IGF-1 deficiency that is not responsive to exogenous GH
SQ injection

SE: hypoglycemia, intracranial hypertension, increased liver enzymes

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12
Q

Octreotide

Lantreotide: long acting formulation for Acromegaly

A

Somatostanin receptor agonist

Used in Acromegaly an several other homone secreting tumors. Acute control of bleeding from esophageal varices

SC or IV injection. Long acting formualtion injected IM

SE: GI disturbances, galsstone, bradycardia, cardiac conduction anomalies

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13
Q

Pegvisomant

A

Blocks GH receptor signalling

USed in acromegaly

SC injection

Increased liver enzymes

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14
Q

Follitropin alfa

A

FSH receptor agonist

Used in controlled ovulation hyperstimualtion in women. Infertility due to hypogonadotropic hypogonadism in men

SC injection

SE: ovarian hyperstimulation syndrome and multiple pregnancies in women. Gynecomastia in men. Headache, depression, edema, in both sexe

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15
Q

Recombinant product with the same peptide sequence as follitropin alfa but differs in its carbohydrate side chains

A

Follitropin beta

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16
Q

Human FSH purified from the urine of postmenopausal women

A

Urofollitropin

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17
Q

Extract of the urine of postmenopausal women; contains both FSH and LH activity

A

Menotropins (hMG)

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18
Q

hCG

A

LH receptor agonist

Initiation of final oocyte maturation and ovulation during controlled ovarian stimulation. Male hypogonadotropic hypogonadism

IM or SC injection

SE: ovarian hyperstimualtion syndrome, multiple pregnancies in women. Gynecomastia in men, headache, depression, edema in both sexes

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19
Q

Recombinant fom of hCG

A

choriogonadotropin alfa

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20
Q

Recombinant form of human LH

A

Lutropin

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21
Q

Leuprolide

A

GnRH receptor agonist

Used in ovarian suppresion. Controlled ovarian stimulation. Central precocious puberty in some transgender early pubertal adolescents. Advanced prostate cancer

Adminsitered IV, SC, IM, or intranasally. Depot formulations are available

SE: headache, light headedness, nausea, injection site reactions, with continuous treatment symptoms of hypogonadism

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22
Q

Synthetic human GnRH

A

Gonadorelin

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23
Q

Ganirelix

A

Antagonist of GnRH receptors

Prevention of premature LH surges during controlled ovarian stimualtion

SC injection

SE: nausea and vomiting

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24
Q

GnRH receptor antagonists approved for prostate cancer

A

Degarelix, abarelix

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25
Bromocriptine
Dopaine D2 receptor agonist Used in hyperprolactinemia, Parkinson's disease Administered orally or for hyperprolactemia, vaginally SE; GI disturbances, orthostatic hypotention, headache, psychiatric disturbances, vasopasm and pulmonary infiltrates in high doses
26
OXytocin
Oxytocin receptor agonist Used in induction and augmentation of labor. Control of uterine hemorrhage after delivery IV infusion SE: fetal distress, placental abruption, uterine rupture, fluid retetion, hypotension
27
Atosiban
Antagonist of oxytocin receptor Tocolysis for preterm labor. IV infusion SE: concern about rates of infant death. not FDA approved
28
Desmopressin
Agonist of vasopressin V2 receptors used in pituitary diabetes insipidus. Hemophilia A and vWF Oral, IV, SC, or intranasal adminsitration SE: GI disturbances, headache, hyponatremia, allergic reactions
29
Used in treatment of DI and sometimes used to control bleeding from esophageal varices?
Vasopressin
30
Conivaptan
Antagonist of vasopressin V1a and V2 receptors used in hyponatremia in hospitalized patients. Administered as an IV infusion Infusion site reactions * Tolvaptan - silimar but more selective for V2 receptors; oral administration limited to 30 day treatment due to hepatoxicity
31
In grave's disease, the cause of the hyperthyroidism is the production of an antibody that \_\_\_\_\_\_\_\_\_\_\_
Activatesthe thyroid gland TSH receptor and stimulates thyroid hormone synthesis and release
32
Methimazole reduces serum concentration of T3 by primarily \_\_\_\_\_\_\_\_\_\_\_\_
Preventing the addition of iodine to tyrosine residues on thyroglobulin
33
A rare but serious toxicity associated with the thioamides
Agranulocytosis
34
A 56 year old woman presented to the emergency deparment with tachycardia, shortness of breath, and chest pain. She had shortness of breath and diarrhea for the last 2 days and was sweating and anxious. a relative reported that the patient had run out of methimazole 2 weeks earlier. The diagnosisof thyroid storm was made. What drug that is sueful adjuvant in the treatment of thyroid storm?
Propanolol
35
What drug can be administered for 10-14 days before surgery to reduce the vasuclarity of the thyroid gland?
Lugol's solution
36
When initiating T4 therapy for an elderly patient with long standing hypothyroidism, it is important to begin with small dosesto avoid \_\_\_\_\_\_
overstimulating of the heart
37
What hormone is produced in the peripheral tissues when levothyroxine is administered??
T3
38
A 62 year old woman presents with complaints of fatigue sluggishness and weight gain. She needs to nap several times. She has been taking T4 for the past 15 years without significant problem regarding her energy level. Her recent history is significant of arrythmia and she is currently taking an anti arrythmic drug. What is the most likely cause of her current situation?
Amiodarone
39
A 25 year old woman presents with insomnia and fears she may habe something wrong with her heart. She describes her heart jumping out of her chest. She feel healthy otherwise and reports she has lots of energy. Lab tests confirms hyperthyroidism. What drug that produces permanent reduction activity?
131I
40
Thyroid preparations | (Levothyroxine, Liothyronine)
Activation of nuclear receptors results in gene expression with RNA formulation and protein synthesis. Hypothyroidism MAximum effect seen after 6-8 weeks of therapy. T4 is converted to T3 in target cells, the liver and the kidneys. T3 is 10x more potent than T4
41
Thiomides | (PTU, methimazole)
Inhibit thyroid peroxidase reactions, iodine organification and peripheral conversion of T4 to T3 Hyperthyroidism Oral administration, delayed onset of activity SE: nausea, GI disturbancs, rash, agranulocytosis, hepatitis (PTU-warning). hypothyroidism
42
Lugol's solution, potassium iodide
Inhibit iodine organification and hormone release. Reduce size and vascularity of thyroid gland Preparation for surgical thyroidectomy Oral adminsitration, acute onset of activity within 2-7 days
43
Radioactive Iodine
Radiation-induced destruction of thyroid parenchyma Used in hyperthyroidism. Patient should be euthyroid or on B-blockers before RAI. Avoid in pregnancy and in nursing mothers Oral adminsitration SE: sore throat, hypothyroidism
44
Beta blockers (Propanolol, other beta blcokers lacking partial agonist activity)
Inhibition of B receptors; Inhibition of conversion of T4 to T3(propanolol only) Used in thyroid storm. adjunct to control tachycardia, hypertension, and atrial fibrillation Rapid onset of activity SE: asthma, AV blockade, hypotension, bradycardia
45
What is the pharmacologic effect of exogenous glucocorticoids in asthma?
Inhibition of leukotriene synthesis
46
One of the adverse metabolic effects of long term glucocorticoid therapy is the ______ of bone, which can result to \_\_\_\_\_\_\_\_
Net loss Osteoporosis
47
A patient is a known case of cushing's syndrome due to adrenal tumor. What drug woul be expected to reduce the signs and symptoms of the patient?
Ketoconazole * Inhibits many types of cytochrome P450 * reduce the unregulated overproduction of corticosteroids by adrenal tumors
48
Describes the therapeutic effect of glucocorticoid administration in patients with 21a-hydroxylase activity
Suppresion of ACTH secretion
49
Describes a glucocorticoid response element
A specific nucleotide sequence that is recognized by steroid hormone receptor-hormone complex
50
Gradual tapering of a glucocorticoid is required for recovery of \_\_\_\_\_\_\_\_\_
The hypothalamic-pituitary-adrenal system
51
Most pont antiinflammatory steroid?
Dexamethasone
52
a 54 year old man has developed signs of severe acute adrenal insufficiency. The patient should be treated immediately with this combination
Cortisol and fludrocortisone
53
Drug that in high doses blocks the glucocorticoid receptor
Mifepristone * Competitive antagonist of glucocorticoid and progesterone receptors
54
Prednisone
Activation of glucocorticoid receptor alters gene transcription Used in may inflammatory conditions, organ transplantation, hematologic cancers Druration of activity is longer than pharmacokinetic half life of drug owing to gene transcription effects SE: adrenal suppression, growth inhibtion, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes
55
Fludrocortisone
Strong agonist at mineralocorticoid receptors and moderate activation of glucocorticoid receptors Used in Adrenal insufficiency (Addison's disease) Lonh duration of action SE: salt and fluid retention, congestive heart failure, signs and symptoms of glucocorticoid excess
56
Mifepristone
Pharmacologic antagonist of glucocorticoid and progesterone receptors Used in MEdical abortion, and very rarely Crushing's syndrome Oral administration SE: Vaginal bleeding in women, abdominal pain, GI upset, diarrhea, headcahe
57
Spironolactone
Pharmacologic antagonist of mineralocorticoid receptor, weak antagonism or androgen receptors Used in aldosteronism from any cause, hypokalemia due to other diuretics, post MI Slow onset and offset of effect. DUration: 24-48h SE: hyperkalemia, gynecomastia (spironolactone, not eplerenone), additive interaction with other K-retaining drugs
58
Eplerenone
More selective for mineralocorticoid receptor similar to spironolactone
59
Ketoconazole
Blocks fungal and mammalian CYP450 enzymes. Inhibits mammalian steroid hormone synthesis and fungal erogosterol syntesis Oral, topical administration SE: hepatic dysfunctio, many drug-dryg CYP450 interactions
60
Beclomethasone and budesonide
readily pentrates the airway mucosa but have short half lives after they enter the bloodm so systemic effects and toxicity are greatly reduced
61
A teenager seeks postcoital contraception. What drug will be effective for this purpose?
Mifepristone * antagonist at progesterone and glucocorticoid receptors * has lutelolytic effect
62
A 23 year old woman desires a combine oral contraceptive for pregnancy protection. What patient factor would lead a health professional to recommend alternative form of contraception?
History of migraine headache that is well controlled by sumatriptan * estrogen containing hormonal contraceptives increases the risk of migraine headcahes
63
Men who uses large doses of anabolic steroids are at increased risk of
Cholestatic jaundice and elevation of AST in the blood
64
A 50 year old woman with a positive mammogram undergoes lumpectomy and a small carcinoma is removed. Biochemical analysis of the cancer reveals the presence of estrogen and progesterone receptors. What drug is recommended for the patient?
Tamoxifen
65
A 60 year old man is found to have a prostate lump and an elevated prostate specific antigen blood test. MRI suggests several enlarged LN in the lower abdomen. and an xray reveals 2 radiolcuent lesions in the bony pelvis. This patient is likely to be treated with \_\_\_\_\_\_
Leuprolide * GnRH agonist used in the treatment of men with prostate cancer * To prevent tumor flares -- add flutamide
66
Most appropriate treatment for endometriosis
Medroxyprogesterone acetate by intramusculat injection
67
DEWS should never be used in pregnant women because it is associated with \_\_\_\_\_
Infertility and developmenmy of vaginal cancer in female offsprine
68
Unique property of SERMs
Act as agonsits in some tissues adn antagonists in other
69
Finasteride has efficacy in the prevention of male-pattern baldness by virtue of its ability to do which of the following?
Reduce the production of dihydrotestosterone * 5a-reductase inhibitor
70
In patients with a strong family of breast cancer ______ may be a better choice than a full estrogen agonist
Raloxifene
71
Ethinyl estradiol
Activation of estrogen receptors leads to changes in the rates of transcription of estrogen-regulated genes USed in hypogonadism in girls, oral and parenteral contraceptive Oral, parenteral, or transdermal adminsitration. metabolism relies on cytochrome P450 systems. Enterohepatic recirculation occurs Side Effects: * Moderate toxicity * Breakthrough bleeding, nasuea, breast tenderness * Serious toxicity * thromboembolism, gallbladder disease, hyperTG, migrane headache, hypertension, depression * In post menopausal women * Breast cancer, endometrial hyperplasia(unopposed estrogen) * Combination with cytochrome P450 inducer can lead to breakthrough bleeding and reduced contraceptive efficacy
72
Prodrug that is converted ti ethinyl estradiol, contained in some contraceptives
Mestranol
73
Long acting estrogens administered IM and used for hypogonadism un young females
Estrogen Esters (Estradiol cypionate)
74
Norgestrel
Activaion of progesterone receptors leads to changes in the rate of transcription of progeterone-regulated genes used in parenteral contraception, postcoital contraceptive Oral, parenteral or transdermal administration, metabolism relies on cytochrome P450. Enterohepatic recirculation occurs SE: weigh gaine, reversible decrease in bone mineral density (high doses)
75
Drospirenone
Spironolactone derivative of norgestrel
76
Tamoxifen
Estrogen antagonist actions in breast tissue and CNS. estrogen agonist effects in liver and bone Used in prevention and adjuvant treatment of hormone-responsice breast cancer Oral administration SE: Hot flushes, thromboembolism, endometrial hyperplasia
77
approved for osteoporosis and prevention of breast cancer in selected patients. **Antagonist** effect in breast, CNS, and endometrium **Agonist** effects in the liver
Raloxifene
78
Approved for treatment of menopausal symptoms and prophylaxis of postmenopausal osteoporosis in combiantion with conjugated estrogens
Bazedoxifene
79
Partial agonist at estrogen receptor; used for ovulation inductionl antagonis effect in pituitary increases gonadotropin secretion
Clomiphene
80
Fulvrestant
Estrogen receptor antagonist in ALL tissues Used in adjuvant treatment of homone-responsive Breast cancer that is resistant to first-line antiestrogen therapy IM adminsitration SE: hot flushes, headaches, injection site reactions
81
Anastrozole
Reduces estrogen synthesis by inhibiting aromatase enzyme Used in adjuvant treatment of hormone responsive breast cancer Oral administration SE: hot flushes, MSK disorders, reduce bone mineral density
82
Irreversible aromatase inhibitor
Exemestane
83
Danazol
Weak cytochrome p450 inhibitor and partial agonist of progestin and androgen receptors Used in endometriosis, fibrocystic breast disease Oral administration. Drug interactions due to cytochrome P450 inhibition SE: acne, hirsutism, weigh gain, menstrual disturbance, heaptic dysfunction
84
Mifepristone
Progestin and glucocorticoid receptor antagonist Used in combination with prostaglandin for medical abortion Oral SE: GI disturbances (mostly due to misoprostol). vatginal bleeding, atypical infection
85
testosterone
Androgen receptor agonist Used in male hypogonadism. weigh gain in patients with wasting syndromes Transdermal, buccal, SQ implant SE: In females, virilization. In men, high doses can cause gynecomastia, testicular shrinkage, infertility
86
Long acting androgens for parenteral administration
Testosterone esters (testosterone cypionate)
87
Anabolic steroids
Oxandrolone, nandrolone decanoate Increased ration of anabolic to androgenic activity in laboratory animals. cholestatic jaundice, liver toxicity
88
Finasteride
Inhibition of 5a-reductase enzume that converts tetosterone to DHT USed in BPH, male pattern hair loss Oral adminisration SE: rarely, impotence, gynecomastia
89
Flutamide
Competitive inhibition of androgen receptor Usedin advance prostate cancer Oral SE: gynecomastia, hot flushes, impotence, hepatotoxicity
90
similar to flutamide but lower risk of hepatotoxicity
Bicalutamide, nilutamide
91
Mineralocorticoid receptor antagonist used mainly as potassium sparing diuretic; also gas androgen receptor antagonist, used for the treatment of hirsutism
Spironoalctone
92
Ketoconazole
inhibition of cytochrome p450 enzymes involved in andrigen synthesis Ued in advanced prostate cancer that is resistant to first line-antiandrogen drugs Oral SE: interferes with synthesis of other steroids. MAny drug interactions due to cytochrome p450 inhibition
93
most likely complication of insulin adminsitration?
hypoglycemia
94
Tight control regimen
Establish a basal level of insulin with a small amount of along acting preparation (Insulin glargine) and supplemeting the insulin levels, when called for by food intake, with short acting insluin (lispro). Lest tight control may be achieved with 2 injections of intermediate acting insulin per day.
95
Glipizide is a second generation ___________ that promotes insulin release by closing potassium channels in the pancreatic B cells
Sulfonylureas
96
Improtant effect of glucose
Increased glucose transport into cells
97
a 54 year old obese patient with type 2 diabetes has a history of alcoholism. In this patient, metformin should either be avoided or used with extreme caution because metformin and ethanol can increase the risk of
Lactic acidosis
98
Drug that is taken during the first part of a meal for the purpose of delaying the absorption of dietary carbohydrates?
Acarbose
99
The PPAR-y receptors that is activated the TZD increases tissue sensitivoty to insulin by\_\_\_\_\_\_\_\_\_\_\_
Regualting transcription of genese involved in glucose utilization
100
\_\_\_\_\_\_\_\_\_ is useful in the treatment of B-blocker induced cardiac depression
Glucagon
101
Rapid acting insulin
Lispro, aspart, glulisine
102
Intermediate actibg insulin
NPH
103
Long acting insulin
Detemir, glargine, degludec
104
Metformin
Decreased endogenous glucose production Used in type2 DM Oral administration SE: GI distubances, lactic acidosis
105
Glipizide
Secretagogues Increases insulin secretion from pancreatic beta cells by closing ATP sensitive potassium channels Used in T2DM Oral SE: hypoglycemia, weight gain
106
Sulfonylureas with intermediate duration of action
Glyburide, glimepiride
107
Fast acting insulin secretatgouges
Repaglinide, nateglinide
108
Acarbose
Alpha glucosidase inhibitors used in T2DM oral SE: GI disturbances
109
Thiazolidinediones | (Rosiglitazone)
Regulatesgene expression by binding to PPAR-y used in type 2 DM Oral administration SE: fluid retention, edema, anemia, weigh gain, bone fracture in women, may worsen heat disease and increase risk of MI
110
Exanatide
Analog of glucagon-like peptide-1 (GLP-1) ParenterGLP-1 Receptors used in T2DM Parenteral SE: Gi disturbances, headache, pancreatitis
111
Sitagliptin
Inhibitor of the DPP-4 that degrades GLP-1 and other incretins Used in T2DM Oral SE: rhiitis, URTI, Rare allergic reactions
112
Pramlintide
Amylin analog used in T1DM and T2DM Parenteral adminsitration SE: GI disturbances, hypoglycemia, headache
113
Glucagon
Activates glucagon receptors Used in severe hypoglycemia and B-blocker overdose PArenteral administation SE: Gi disturbances, hypotension
114
SGLT2 inhibitors | (Canaglifozin, dapaglifozin)
Inhibit renal glucose absorption via SGLT2 used in T2DM Oral SE: Osmotic diuresis, genital and urinary tract infections
115
What drug is routinely added to calcium supplements?
Cholecalciferol
116
Most useful for the treatment of hypercalcemia in Paget's disease
Pamindronate * Biphosphonates and calcitonin are first line treaments * Paminodranate can be given pareneterally
117
The active metabolites of vitamin D act through a nuclear receptor to produce this effect
Increase the absorption of calcium from the gastrointestinal tract
118
\_\_\_\_\_\_\_\_\_ increases bone formation and bone resoprion
Teriparatide Should not be used longer than 2 years due to risk of osteosarcoma.
119
Long erm therapy 0f ___________ is assocaited with reduction in bone mineral density and an increased risk of fractures
Glucocorticoids
120
Oral biphosphontes can cause \_\_\_\_\_\_\_\_\_\_\_
erosive esophagitis
121
\_\_\_\_\_\_\_\_\_ is a peptide hormone that prevents bone resorption. Can be given as nasal spray
Calcitonin (Salmon calcitonin is available as nasal spray)
122
In aptients with chronic kidney disease that requires dialysis, the impaired priduction of active vitamin D metabolities with elevated serum phosphate due to renal impairment leads to secondary hypePTH. Administration of ___________ is necessary
Calcitriol
123
\_\_\_\_\_\_\_\_\_ is an analog of 1,25 dihydroxyvitamin D3 that lowers serum PTH at doses that rarely precipitate hypercalcemia
Paricalcitol
124
MOA of cincalcet as PTH lowering agent
Activating the serum sensing receptor in PTH cells
125
Vitamin D metabolites, analogs | (Cholecalciferol, ergocalciferol)
Regulates gene transcription via the vitamin D receptor to produce the effect Used in vitamin D deficiency, osteoporosis, osteomalacia, psoriasis Oral adminsitration.requires metabolism in the liver or kindey to active forms SE: hypercalcemia, hyperphosphatemia, hypercalciuria
126
Used for management of secondary hyperPTH in patients with chronic kidney disease and for management of hypercalcemia in patients with hypoPth.
Cacitriol this drug is in its active form
127
an analog of calcitriol approved for psoriasis
Calcipotriene
128
Alendronate
Suppresses the activity of osteoclasts and inhibits bone resorption Used in Osteoporosis, Paget's disease Oral adminsitration daily or weekly SE: adynamic bone, esophageal irritation, osteonecrosis of the jaw (rare)
129
Teriparatide
PTH analog Acts throught PTH receptors to produce a netr increase in bone formation Used in Osteoporosis SQ inhection SE: hypercalcemia, hypercaliuria, osteosarcoma in experimental animals
130
full length rhPTH used for hypoPTH
Natpara
131
Calcitonin
Acts through calcitonin receptors to inhibit bone resorption. Used in osteoporosis SQ or intranasal SE: rhinitis with the nasal spray
132
Raloxifene
Estrogen agonist effect in bone. Estrogen antagonist effects in breast and endometrium Osteoporosis in post menopausal women Oral adminsitration SE: Hot flushes, Thromboembolism
133
Denosumab
Binds to TANKL an prevents it from stimulating osteoclasts differentiation and function Used in osteoporosis SQ every 6 months SE: may increase risk of infections, osteonecrosis of the jaw (rare)
134
Cinacalcet
Actiavates the calcium sensing receptor Used in hyperparathyroidism Oral adminsitration SE: nausea, hypocalcemia, adynamic bone
135
Minerals | (calcium phosphate strontium)
Strontium suppresses bone resorption and phosphate required for bone mineralization Used in osteoporosis, osteomalacia, calcium or phosphate deficiencies Oral and parenteral SE: ectopic calcification