Endocrine Pharmacology Flashcards Preview

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Flashcards in Endocrine Pharmacology Deck (150):
1

Hormones from the Anterior Pituitary

GH
Gonadotropins
Prolactin

2

Hormones from the Hypothalamus

GnRH

3

Hormones from the Posterior Pituitary

Oxytocin
Vasopressin

4

GH Inhibitor

Somatostatin

5

PRL Inhibitor

Dopamine

6

Mediator of GH

IGF-1

7

Mediators of TSH

Thyroxine
Triiodothyronine

8

Mediators of ACTH

Glucocorticoid
Mineralocorticoid
Androgens

9

Mediators of FSH/LH

Estrogen
Progesterone
Testosterone

10

Increases release of IGF1
Hormone for GH deficiency, short stature, Failure to thrive, AIDS wasting

Somatotropin

11

Drug used for performance enhancement (increases muscle mass), banned by athletics committees

Somatotropin

12

Somatostatin analog
Suppresses secretion of GH, IGF1, Serotonin and GI peptides
Drug for acromegaly, pituitary adenoma (GH secreting), carcinoid, gastrinoma, glucagonoma, variceal bleeding
Can alter requirements for antidiabetic agents

Octreotide
(Lanreotide)

13

In women, FSH directs_____; while FSH and LH collaborate for _________

follicle development
ovarian steroidogenesis

14

In men FSH regulates______ and LH stimulates_________.

spermatogenesis
androgen production

15

Ovulation induction can cause ovarian hyperstimulation syndrome with the following triad of Sx:

Ovarian Enlargement
Hypovolemia
Ascites
Possibly Shock

16

FSH Analog
Drug for controlled ovarian hyperstimulation, infertility due to hypogonadism in men
SE: Ovarian Hyperstimulation syndrome, multiple pregnancies, gynecomastia in men

Follitropin Alfa
(Menotropins (hMG), UROFOLLITROPIN (from urine of menopausal women), Follitropin Beta)

17

LH Analog
Drug for controlled ovarian hyperstimulation, hypogonadotropic hypogonadism
SE: Ovarian hyperstimulation syndrome, multiple pregnancies, gynecomastia in men

Choriogonadotropin Alfa
(HUMAN CHORIONIC GONADOTROPIN (hCG), Menotropins (hMG), Lutropin

18

Increased LH and FSH secretion with intermittent administration, reduced LH and FSH with continuous administration
Drug for Controlled ovarian hyperstimulation, endometriosis, myoma uteri, precocious puberty, prostate cancer
SE: Hot flushes, osteoporosis, gynecomastia, temporary exacerbation of precocious puberty or prostate cancer

Leuprolide

LAHAT NG -RELIN

19

GnRH Antagonist
Drug for Controlled Ovarian Hyperstimulation, Prostate Cancer
SE: Hypersensitivity (Abarelix)
Does not cause tumor flare up when used for prostate cancer

Ganirelix

LAHAT NG -RELIX

20

Partial D2 receptor agonist
Inhibits GH release
Drug for hyperprolactinemia, Pituitary adenoma (PRL secreting), acromegaly, Parkinson's
SE: Erythromelalgia, Reynaud's Phenomenon, Pulmonary infiltrates

Bromocriptine
(Pergolide, Carbergoline, Quinagolide)

21

Stimulates uterine contraction and labor
Stimulates milk letdown
Drug for labor induction/augmentation, control of postpartum hemorrhage
SE: Fetal distress, placental abruption, uterine rupture, water intoxication, hypotension

Oxytocin

22

Contraindications to Oxytocin

Fetal distress
Prematurity
Abnormal Presentation
CPD
Predispositions for uterine rupture

23

Vasopressin V2 receptor agonist
DOC for Central DI

Desmopressin
(Vasopressin)

24

Sx of Central DI

Polyuria
Polydipsia
Hypernatremia
Inability to resorb water from the urine

25

Central DI: deficient _________ of ADH
Nerphrogenic DI: end-organ ________ to ADH

Secretion
Resistance

26

Antagonist at V1a and V2 receptors
Drug for SIADH
Central Pontine Myelinosis may occur with rapid correction of hyponatremia

Conivaptan
(Tolvaptan, Lixivaptan)

27

T3 is about ______ times more potent than T4

10

28

T___ is converte to T____ in target cells

T4 to T3

29

Identify if Thyrotoxicosis or Hypothyroidism:
Weakness
Increased DTR
Menstrual Irregularity
Decreased Fertility

Thyrotoxicosis

30

Identify if Thyrotoxicosis or Hypothyroidism:
Stiffness
Decreased DTR
Infertility
Decreased Libido
Impotence
Oligospermia

Hypothyroidism

31

Thyroid hormone
Activation of nuclear receptors
Drug for Hypothyroidism, Myxedema Coma
SE: Dry skin, nervousness, heat intolerance

Levothyroxine (T4)
Liothyronine (T3)

32

T4 dose must be lowered in pxs with __________ or longstanding __________ due to increased cardiosensitivity

Cardiovascular disease
Hypothyroidism

33

Thioamide
Inhibits Thyroid peroxidase
Blocks peripheral conversion of T4 to T3
Drug for Hyperthyroidism (esp in Pregnant), Thyroid Storm
SE: Fulminant hepatitis, Agranulocytosis
Slow onset of action (3-4 weeks for full effect)
Largely protein bound

PTU

34

Thioamide
Inhibits Thyroid peroxidase, blocks iodine organification
Drug for hyperthyroidism (DOC in nonpregnant)
SE: Cholestatic jaundice, agranulocytosis
altered sense of taste/smell
Slow onset of action (3-4 weeks for full effect)

Methimazole

35

Prenatal exposure to Methimazole can lead to this condition

Aplasia Cutis Congenita
(Absence of a portion of skin in a localized or widespread area at birth)

36

Sx of Agranulocytosis

Acute severe neutropenia
sore throat or high fever
increased susceptibility to infections

37

Tx for Agranulocytosis

Give G-CSF to stimulate body to make more WBC
Discontinue medication

38

Iodide
Emits beta rays causing destruction of thyroid parenchyma
Hyperthyroidism
SE: Permanent hypothyroidism
Preferred treatment for most patients
Contraindicated in pregnant women or nursing mothers

Radioactive Iodine 131I

39

Iodide
Inhibits iodine organification, reduces size and vascularity of thyroid gland
Drug for thyroid storm, hyperthyroidims, preop thyroidectomy, radiation prophylaxis
SE: Iodism, metallic taste
Prevents radiation induced thyroid damage
Should not be used alone (escape in 2-8weeks)

Potassium Iodide
Lugol's Solution

40

Prenatal exposure to Potassium Iodide can cause _____

Fetal Goiter

41

Identify: Ingestion of Iodine causes Hypothyroidism

Wolf-Chaikoff Effect

42

Identify: Ingestion of Iodine causes Hyperthyroidism

Jod-Basedow Effect

43

This drug causes clinical improvement of hyperthyroidism without altering thyroid hormone levels

Class?

Beta Blockers

44

This beta blocker may be used to treat thyrotoxicosis-related arrhythmia

Esmolol

45

Enumerate the anti-thyroid drugs that inhibit peripheral conversion of T4 to T3

Propylthiouracil
Propranolol
Hydrocortisone
Contrast with Iodine
Methimazole

46

Granulocyte count of <500cells/mm3
Sudden acute exacerbation of all the symptoms of thyrotoxicosis

Thyroid Storm

47

Tx of Thyroid Storm

PTU (inhibits conversion of iodide to iodine)
Iodides
Propranolol
Hydrocortisone (protects against shock)

48

Drugs that can induce Hyperthyroidism

Clofibrate
Amiodarone (can convert T4 to T3, or iodine induced in a person with underlying thyroid disease, or inflammatory causing leakage of thyroid hormone)
Methadone

CAM

49

Tx for Amiodarone induced Thyroid Disease due to Peripheral Conversion

Levothyroxine

50

Tx for Amiodarone induced Thyroid Disease due to Iodine-induced mechanism in those with underlying thyroid disease or inflammatory causing leakage of thyroid hormone

Thioamides (PTU/Methimazole)
Corticosteroids

51

Common Precursor of Corticosteroids

Cholesterol

52

Short-acting, low potency glucocorticoid
Suppresses inflammation
Drug for adrenal insufficiency, insect bites, contact dermatitis, status asthmaticus, thyroid storm

Hydrocortisone
Low Potency: Desonide
Medium Potency: Fluticasone, Mometasone
High Potency: Desoximetasone, Clobetasol

53

Glucocorticoid
SE: Adrenal SUPPRESSION

Prednisone
(Betamethasone, Triamcinolone, Dexamethasone)

54

This glucocorticoid hastens fetal lung maturation

Betamethasone

55

Mineralocorticoid
Strong agonist, moderate anti-inflammatory effects
Drug for chronic adrenal insufficiency (Addison's Disease), Congenital Adrenal Hyperplasia, Adrenal Replacement Therapy Post-Adrenalectomy
SE: Salt and fluid retention, HypoK, Congestive HF
Additive HypoK with Loop diuretics and thiazides

Fludrocortisone
(Deoxycorticosterone)

56

Destruction or dysfunction of entire adrenal cortex
Ususally symptomatic only with >90% destruction

Addison Disease

57

Adrenal Insufficiency is what syndrome?

Addison

ADDrenal insuficiency

58

Adrenal Excess is what syndrome?

Conn

exCess

59

Most common cause of Iatrogenic Cushing Syndrome

Exogenous Steroid Intake

60

Most common cause of Adrenal Cushing Syndrome

Cortisol Secreting Adrenal Adenoma

61

Most common cause of Pituitary Cushing Syndrome

ACTH-secreting Pituitary Adenoma

62

Most common cause of Ectopic Cushing Syndrome

Paraneoplastic ACTH production from lung tumors

63

Glucocorticoid Synthesis Inhibitor
Inhibits DESMOLASE, blocking conversion of cholesterol to prenenolone
Drug for breast cancer, cushing syndrome
Abused by body builders to lower circulating cortisol in the body and prevent muscle loss

Aminoglutethamide

64

Glucocorticoid synthesis inhibitor, Antifungal
Inhibits cholesterol side chain cleavage
Drug for fungal infection
SE: Hepatotoxicity, Gynecomastia, GI disurbances
Inhibitor of CYP450

Ketoconazole

65

Glucocorticoid Synthesis Inhibitor
Inhibits 11-hydroxylation
Drug for diagnostic testing, Cushing syndrome
DOC for pregnant patients with cushing's syndrome

Metyrapone

66

This hormone derived from horses is used for HRT

Premarin

67

Estrogen
SE: Breakthrough bleeding, breast tenderness, HyperTG, HPN
Increases risk for endometrial CA and breast CA (prevented by combining with progestin)

Ethinyl Estradiol
(Mestranol, Estradiol Cypionate)

68

Synthetic estrogen (nonsteroid)
Drug for metastatic prostate cancer
SE: Increased incidence of Clear Cell Adenocarcinoma in daughters of mothers who took this drug

Diethylstilbestrol

69

Progestin
SE: Decreased HDL, Weight gain, Reversible decrease in bone mineral density
Prevents estrogen induced endometrial cancer when used in combination

Norgestrel
(Megestrol, Ethynodiol, Desogestrel, Etonogestrel)

LAHAT NG MAY NOR-

70

Type of Oral Contraceptive:
Taken in constant dosage

Monophasic

71

Progestin or Estrogen Dosage changes during the month

Biphasic or Triphasic

72

Contraceptives may be given within ______ hours after unprotected intercourse

72hours

73

MOA of Combination Hormonal Contraceptives

Inhibition of Ovulation

74

COC
Activates estrogen and progesterone receptors
SE: Breakthrough bleeding, DVT, Breast CA

Estradiol + Norethindrone
(Ethinyl Estradiol PLUS: Desogestrel/Norgestrel, Drospirenone, Norgestimate

75

Does not protect against STDs

Pills

76

POP
Alters cervical mucus and creates a hostile endometrium
SE: Breakthrough bleeding, Delayed return of fertility, Osteoporosis

Medroxyprogesterone Acetate

IM preparation (Depo-provera)

77

Post coital contraceptive
SE: Severe nausea, dizziness
Must be taken within 72 hours of unprotected sexual intercourse

Levonorgestrel

78

_____ Regimen is for emergency contraception

Yuzpe
4 tabs OCP then 4 tabs again after 12 hours

79

Mixed estrogen agonists that have agonist effects in some tissues and antagonists in others
Class?

SERMs

80

Estrogen antagonist in breast tissue and CNS
Estrogen agonist in uterus
Drug for Hormone Responsive Breast CA (ER+/PR+)
Prevents osteroporosis and decreases risk of atherosclerosis at the risk of causing endometrial CA
Drug?

Tamoxifen
TAnggal Mammary Mo = TAMOxifen

81

Estrogen Antagonist in Breast, Uterus and CNS
DDrug for Osteoporosis and Breast CA PREVENTION
Reduces risk of Breast CA in those who are VERY HIGH RISK
No estrogenic effects on endometrial tissue

Raloxifene

82

Partial estrogen agonist in pituitary
Reduces negative feedback by estradiol
Increases FSH and LSH output
Drug for induction of Ovulation
SE: Ovarial enlargement, multiple pregnancies

Clomiphene

Clone Me Phlease

83

Aromatase inhibitor
Drug for Breast CA, Precocious puberty
Effective to tamoxifen resistant Breast CA

Anastrozole
(Letrozole, Exemestane)

Aromatase inhibits Testosterone to Estrogen

84

Partial agonist of Progestin and Androgen receptors
Drug for Endometriosis, Fibrocystic disease
SE: Weight gain
Contraindicated during pregnancy and breast-feeding

Danazol
(Anti-androgen)

85

Antagonist of glucocorticoid and progesterone receptors
Drug for medical abortion
Combination with Misoprostol results in abortion of 95% of early pregnancies
May cause sepsis from unusual organisms

Mifepristone (RU-486)

Organisms like Clostridium Sordeli

86

Active form of Testosterone in Prostate

DHT
DIhydrotestosterone

87

Stimulate RBC production in certain anemias
Promotes weight gain
Performance enhancement in athletes
Drug?

Testosterone

88

Androgen
Increases muscle bulk and RBC production
Drug for male hypogonadism, wasting syndromes in AIDS
SE: Virilization in females, paradoxical feminization in males
Contraindicated in pregnant women and patients with prostate cancer

Testosterone

LAHAT NG MAY -TERONE

89

Anabolic steroid androgen
Increases ratio of anabolic to androgenic activity
Drug for performance enhancement
SE: Virilization in females, Paradoxical feminization in males, Cholestatic jaundice, Elevated liver enzymes, HCC

Oxandrolone

LAHAT NG MAY -ANDROLONE

90

Androgen antagonist
Drug for prostate cancer (prevention of acute flare up), surgical castration (Nilutamide)

Flutamide
(Bicalutamide, Nilutamide)

Fake Androgen: Flutamide

91

Less hepatotoxicity with which androgen antagonists?

Bicalutamide
Nilutamide

92

Must be co-administered with Leuprolide to prevent prostate cancer flare up

Flutamide

Fake Androgen: Flutamide

93

Androgen antagonist
Drug for hirsutism, decreases sexual drive in men
Currently an orphan drug

Cyproterone
(Cyproterone Acetate)

94

Androgen synthesis inhibitor
Inhibits 5alpha-reductase converting testosterone to DHT
Drug for BPH, male pattern baldness, hirsutism
SE: Impotence
Controversial use in prostate cancer

Finasteride

LAHAT NG -ASTERIDE

FinAsteRIde: Five Alpha Reductase Inhibitor

95

C peptide is used to:

differentiate Type 1 and Type 2 DM
Diagnose MEN
Rule out factitious hypoglycemia
Assess insulin resistance

96

MOA of Insulin

Binds to tyrosine kinase receptor
Activates phosphatidylinositol-3-kinase and MAP kinase
Translucation of glucose transporters

97

Rapid Insulin, duration is 3-4 hours

Lispro
Aspart
Glulisin

mabiLIS!

98

Short Acting Insulin, duration is 5-7 hours

Regular

99

Intermediate-Acting Insulin, duration is 18-24 hours

NPH
Lente

100

Long-Acting Insulin, duration is 18-24 hours

Ultralente

101

Ultralong Acting Insulin, duration is >24 hours

Glargine : go LARGe!
Detemir
Lantus: LANTa na sa sobrang tagal

102

Paradoxical improvement f Diabetes in ESRD is due to?

Prolonged half-life of insulin due to decreased clearance

103

These symptoms are results of CNS deprivation

Neuroglycopenic Symptoms

104

Thes symptoms are results of CNS mediated sympathoadrenal discharge

Neurogenic (or Autonomic) Symptoms

105

Patients who are more prone to developing hypoglycemia with insulin:

Advanced renal disease
Elderly
Children below 7 years

106

Identify Effect and Tx:
Evening dose is High
3AM is low
7AM is high

Somogyi
Decrease Insulin

107

Identify Effect and Tx:
Evening dose is Low
3AM is high
7AM is high

Waning
Increase Insulin

108

Identify Effect and Tx:
3AM is Normal
7AM is high (mild)

Dawn Phenomenon
Insulin sensitivity becomes low between 6am and 7am due to GH spike

109

Identify Effect and Tx:
Evening dose is High
3AM is high
7AM is higher

Waning + Dawn Phenomenon
Increase Insulin

110

Period when exogenous insulin requirements decrease due to an increase in endogenous production of insulin
This is followed by a TOTAL LACK of endogenous insulin

Honeymoon Period

111

Most physiologic strategy for Insulin Therapy

Basal Bolus

Long acting BASAL + Short acting BOLUS with every meal

112

Amount of short-acting insulin is varied depending on pre-prandial CBG

Sliding Insulin Scale

113

Only routes for administration of Insulin

Subcutaneous
IV

Inhalational seems promising

114

MOA of insulin Secretagogues

closure of K channels in Pancreatic B cell membrane
Not effective in Pxs who lack functional pancreatic B cells
Requires Islet Cell Function

115

1st Generation Sulfonylurea
SE: Hypoglycemia, Weight Gain, Disulfiram Reaction, Dilutional Hyponatremia
Drugs that compete for protein binding may enhance hypoglycemic effects
Requires islet cell function

Chlorpropamide

LAHAT NG -AMIDE
(Except Gibenclamide)

116

2nd Generation Sulfonylurea
SE: Hypoglycemia (less), Weight Gain, Cholestatic Jaundice (Glibenclamide)
Contraindicated with hepatic impairment and renal insufficiency
Requires Islet cell function

Glipizide

LAHAT NG GLI-

117

Meglitinide
Insulin Secretagogue
For Postprandial hyperglycemia
SE: Hypoglycemia (least), Upper Respiratory Tract Infections
Used in Diabetics with Sulfa Allergies
Nateglinide has the least Incidence of hypoglycemia and may be used in CKD patients
Requires islet cell function

Repaglinide

LAHAT NG -GLINIDE

118

MOA of Biguanides

Reduces fasting and postprandial glucose levels
inhibition of hepatic and renal gluconeogenesis
stimulates glucose uptake and glycolysis in peripheral tissues

119

First line for T2DM (esp Obese)
Inhibits hepatic and renal gluconeogenesis
SE: Weight loss, Lactic acidosis, Vit B12 malabsorption
Contraindicated in pxs with renal disease, alcoholism, hepatic disease, or conditions with tissue anoxia

Metformin

120

MOA of Thiazolidinediones

Increases target tissue sensitivity to insulin
Reduces fasting and post-prandial glucose
Increases glucose uptake in muscle and adipose
Inhibits hepatic gluconeogenesis

121

Thiazolidinedione
Regulates gene expression, binds to PPAR-gamma
SE: Fluid retention, congestive heart failure, Dec HDL, Inc LDL, Inc TG
Contraindicated in pregnancy, chronic liver disease, Congestive heart failure

Pioglitazone

LAHAT NG -GLITAZONE

122

Anti-diabetes drug that reduces mortality and macrovascular events (MI/Stroke)

Pioglitazone

123

MOA of Alpha Glucosidase Inhibitors

Important for the conversion of complex carbs to monosaccharides
Reduction of post-prandial hyperglycemia
Lacks an effect on Fasting Blood Sugar
Reduces risk of Diabetes on High Risk Pxs

124

Inhibits Intestinal Alpha Glucosidases
Drug for Diabetes prevention
SE: GI disturbance, Flatulence, Hypoglycemia with sulfonylureas
Minor glucose lowering benefit
Contraindicated in pxs with renal impairment

Acarbose
(Miglitol, Voglibose)

Adjunct therapy only

125

Novel Diabetic Agents

Pramlintide
Exenatide
Sitagliptin

126

Amylin analog
Suppresses glucagon release, delays gastric emptying, reduces appetite
Administered as injectable solution with insulin

Pramlintide

127

Incretin modulator, GLP-1 Agonist
Retards Gastric Emptying, Inhibits glucagon secretion, Produces SATIETY
SE: Hypoglycemia
Administered as an injectable preparation used in combination with metformin or a sulfonylurea

Exenatide

128

Incretin modulator, DPP-4 Inhibitor (degrades GLP1)
Administered orally as monotherapy or in combination with metformin

Sitagliptin

129

Inhibits GI and pancreatic lipase, reduces fat absorption
Drug for Obesity and T2DM
SE: Weight loss, Steatorrhea
Rebound weight gain, contraindicated in pregnancy, malabsorption

Orlistat

130

Inhibits NE and serotonin reuptake in the CNS, reduces appetite
Drug for Obesity
SE Anticholinergic effects
Withdrawn due to increased risk of cardiovascular events and strokes

Sibutramine
(Reductil)

131

Selectively blocks cannabinoid 1 receptors, reduces appetite
Drug for Obesity
SE: Suicidality, depression, nausea
Withdrawn due to increased risk of suicides, depression

Rimonabant

132

Contents of Bangkok Pills and adverse effect

Ephedrine
Fenfluramine
Phentermine

Adverse effect: Valvular Heart Disease

133

MOA of Glucagon

Catabolic
Increases heart rate and force of contraction
increases hepatic glycogenolysis and gluconeogenesis
Relaxes smooth muscles

134

Activates glucagon receptors
Drug for severe hypoglycemia, beta blocker overdose

Glucagon

135

These tumors present with decreased AA in blood, anemia, diarrhea, weight loss and NECROLYTIC MIGRATORY ERYTHEMA

Glucagonoma

136

MOA of PTH

Increase bone turnover, hypercalcemia, hyperphosphatemia

137

This electrolyte regulates the synthesis and secretion of PTH

Free Ionized Calcium

138

Recombinant PTH
Drug for Osteoporosis
Must be administered in low intermittent dses to stimulate bone formation

Teriparatide

139

Sx of excess Parathyroid Hormone

Painful bones
Renal stones
Abdominal groans
Psychiatric overtones

140

Effect of PTH on Phos

Phosphate
Thrashing
Hormone

141

IIndirectly increases calcium and phosphate absorption in the intestine via Increasing Vit D metabolites
Decreased calcium excretion, increase Phos excretion in the kidne
Increased Ca and Phos resorption in bone
Serum calcium increased, serum phosphate decreased

PTH

142

Increased calcium and phosphate absorption
Increased resorption of calcium
Increase Ca and Phos resorption, promoting mineralization
Serum Ca and Phos both increased

Active Vit. D Metabolytes

143

Inactive Vit D
Stimulates INtestinal Ca absorption, bone resorption, renal Ca and Phos reabsorption
Drug for Vit D deficiency
This is added to dairy products

Ergocalciferol

LAHAT NG -CALCIFEROL

144

Active Vit D
Drug for secondary hyperparathyroidism in CKD, Psoriasis
This is required in CKD, liver disease and hypoparathyroidism

Calcitriol

145

Hormone secreted by Parafollicular C cells in the Thyroid Gland
Decreases Serum Ca and Phos by inhibiting bone resorption and inhibiting renal excretion of Ca and Phos

Calcitonin

(Tones down Calcium, Reverses PTH)

146

Drug for Paget Disease of Bone, Hypercalcemia, Osteoporosis, Tumor marker of thyroid cancer
Given as nasal spray

Calcitonin

LAHAT NG - TONIN

147

Excessive bone resorption leading to formation of weaker bones

Paget Disease of Bone

148

Bisphosphonate
Suppresses Osteoclast activity
Drug for Paget disease of bone, hypercalcemia, osteoporosis
SE: Adynamic bone, Esophagitis, Osteonecrosis of the jaw

Alendronate

LAHAT NG -DRONATE / -DRONIC ACID

149

Take this drug with large quantities of water
Contraindicated in renal impairment, esophageal motility disorder and PUD

Alendronate

150

Phosphate binding resin
Binds to dietary phosphate and prevents absorption
Drug for hyperphosphatemia in CKD
Can reduce Uric Acid levels
Contraindicated in HYPOphosphatemia and bowel obstruction

SEVELAMER

Tablets rapidly expand