Drugs to Know Endocrine

Octreotide Brand Name

Sandostatin

Octreotide Indication

treats carcinoid (metastatic neuroendocrine tumor) syndrome (flashing, diarrhea)

Octreotide Side Effects

Gastrointestinal - diarrhea, nausea, abdominal pain (50%), gallstones (25%)

Cardiac - sinus bradycardia, conduction disturbance

Lanreotide Brand Name

Somatuline

Lanreotide Indication

Prolonged GH suppression

Lanreotide and Octreotide Warnings and Precautions

Gallstones

Glucose Monitoring - (hypo and hyperglycemia can occur

Cardiac: bradycardia, arrhythmia

Thyroid function: hypothyroidism possible

Lanreotide and Octreotide Drug interactions

Diabetes drugs, cyclosporine, beta blockers, bromocriptine

Pegvisomant Brand Name

Somavert

Pegvisomant Mechanism of Action

binds very tightly to one GHR in the GHR-homodimer

Does not lead to signaling through JAK and blocks native GH from binding to the GHR (competitive agonist)

Pegvisomant Warnings and Precautions

monitor liver function

Pegvisomant drug interactions

diabetes drugs (dose reduction to avoid hypoglycemia)

Opioids: patients on opioids may need higher doses to achieve appropriate IGF-1 suppression

Somatotropin Brand Name

Serostim

Somatotropin Mechanism of Action

Activates GH-R

increases body growth and general anabolic

Somatotropin Indication

GH deficiency

HIV vesting

Short bowel syndrome

Somatotropin Warnings and Precautions

contraindicated in cancer patients

Mecasermin brand name

Increlex

Mecasermin mechanism of action

Activates IGF-1 receptors

increases growth and anabolic effects

Mecasermin indication

IGF-1 replacement

Mecasermin warnings and precautions

hypoglycemia

Somatostatin receptor agonists

Octreotide and Lanreotide

Growth Factor receptor antagonists

Pegvisomant

Growth factor receptor agonists

Somatotropin

Somapacitan-beco (Sogroya)

Lonapegsomatropin-tcgd (Skytrofa)

Gonadotropin-releasing hormone receptor agonists

Leuprolide (Lupron)

Goserelin (Zaladex)

CHEMICALLY SYNTHESIZED ANALOGS

Leuprolide Brand Name

Lupron

Goserelin Brand Name

Zaladex

Leuprolide & Goserelin Mechanism of Action

Activates GnRH receptors

increases or decreases FSH and LH production, depending on the dosing patternL

Leuprolide & Goserelin Indication

prostate cancer

puberty control

ovarian stimulation/suppression

Leuprolide & Goserelin warnings and precautions

hypogonadism if used continuously

Gonadotropin releasing hormone receptor agonists (Identical to native sequence)

GnRH

Gonadorelin

Identical to chemically synthesized analogs

Gonadotropin-releasing hormone receptor antagonists

Ganirelix (Orgalutran)

Cetrorelix (Cetrotide)

Ganirelix Brand Name

Orgalutran

Cetrorelix Brand Name

Cetrotide

Ganirelix & Cetrorelix mechanism of action

inhibits GnRH receptors

decreases FSH and LH release

Ganirelix & Cetrorelix indication

fertility treatment (not common anymore)

Follicle-stimulating hormone

Follitropin (Gonal-f)

Urofollitropin (Bravelle)

Follitropin Brand Name

Gonal-f

Follitropin & Urofollitropin mechanism of action

activates FSH receptors

identical to native FSH

Follitropin & Urofollitropin indication

fertility treatment

Follitropin & Urofollitropin warnings and precautions

Gynecomastia in men

Ovarian hyperstimulation

Urofollitropin Brand Name

Bravelle

Luteinizing Hormone

Lutropin (Luveris)

Lutropin Brand Name

Luveris

Lutropin mechanism of action

Activates LHCG receptors

identical to native LH

Lutropin indication

fertility treatment

Lutropin warnings and precautions

ovarian hyperstimulation

Choriogonadotropins

Ovidrel

Pregnyl

Ovidrel & Pregnyl Mechanism of Action

Activates LHGC receptors

identical to hCG (both)

Ovidrel & Pregnyl Indication

fertility treatment

FSH & LH mixtures

Menotropins

Menotropins mechanism of action

Activates FSH & LHCG receptors

identical to FSH & LH

Menotropins indication

fertility treatment

Dopamine (D2) receptor agonist

Bromocriptine (Cycloset)

Bromocriptine Brand Name

Cycloset

Bromocriptine Mechanism of Action

Activates dopamine D2 receptors (CNS motor effects)

Suppresses prolactin and (less effective) GH release

Bromocriptine indication

Hyperprolactinemia

Acromegaly

(Parkinson’s)

Oxytocin receptor agonist

Oxytocin (Pitocin)

Oxytocin Mechanism of Action

Activates oxytocin receptor

Increases uterine contractions

Oxytocin Indication

Labor induction

Oxytocin Warnings and Precautions

fetal stress, placental rapture

Vasopressin receptor agonists

Vasopressin (Vasostrict)

Desmopressin (DDAVP)

Vasopressin Brand Name

Vasostrict

Desmopressin Brand Name

DDVAP

Desmopressin & Vasopressin Mechanism of Action

activates preferentially V1R vasopressin receptor & increases blood pressure (Vasopressin)

Activates preferentially V3R vasopressin receptor & decreases water excretion by kidney (desmopressin)

Vasopressin Indication

Vasodilatory shock

Desmopressin Indication

Pituitary diabetes insipidus

Vasopressin Warnings and Precautions

monitor cardiac function

Desmopressin Warnings and Precautions

Gi disturbances, hyponatremia

Thyrotropin releasing hormone receptor agonists

TRH (Protirelin)

TRH Brand Name

Protirelin

TRH Mechanism of Action

TRH-receptor agonist

increases thyrotropin release

TRH Indication

Diagnostic

Thyrotropin Receptor Agonist

Thyrotropin (TSH)

Thyrotropin Mechanism of Action

TSH receptor agonist

Increases thyroid hormone levels

Thyroid Hormone T4

Levothyroxine (Synthroid)L

Levothyroxine Brand Name

Synthroid

Levothyroxine & Liothyronine Mechanism of Action

binds to the nuclear thyroid hormone receptor

Regulates gene expression

Levothyroxine Indication

hypothyroidism, T4 replacement

Thyroid Hormone T3

Liothyronine (Cytomel)

Liothyronine Brand Name

Cytomel

Liothyronine Indication

Hypothyroidism, T3 replacement

Liothyronine & Levothyroxine Warnings and Precautions

Hyperthyroidism

Thioamides

Methimazole (Northyx)

Propylthiouracil (Propycil)

Methimazole & Propylthiouracil Mechanism of Action

inhibits thyroid peroxidase

decreases thyroid hormone levels

Methimazole & Propylthiouracil Indication

hyperthyroidism

Methimazole & Propylthiouracil Warnings and Precautions

hypothyroidism

Iodides

Iodide solutions, pills, Lugol

Iodide solutions, pills, Lugol Mechanism of Action

inhibits organification and hormone release

decreases thyroid hormone levels

Iodide Indication

hyperthyroidism, pre-surgery preparation

Radioactive iodide

Iodide 131I (B-emitter)

131I (B-emitter) Mechanism of Action

Accumulates in the thyroid

tissue destruction

131I indication

radiotherapy

Glucocorticoids

Hydrocortisone, Cortisone, Prednisolone, Methylprednisolone, Triamcinolone, Dexamethasone, Betamethasone

Hydrocortisone Brand Name

Solu-Cortef

Cortisone Brand Name

Hydrocort

Prednisolone Brand Name

Omnipred

Methylprednisolone Brand Name

Medrol

Triamcinolone Brand Name

Kenalog

Dexamethasone Brand Name

Dexasone, Decadron

Betamethasone Brand Name

Celestone

Glucocorticoids Mechanism of Action

Activates glucocorticoid receptors

Hormone replacement, anti-inflammatory, and immunosuppressive properties