Endocrine System Drugs

Drug Name	IUPAC Name	Classification (KD Tripathi)	Drug Application	Receptors	Dosage Form	Route of Administration	Adverse Reactions	Appearance	Solubility	pKa Value	Functional Groups
Levothyroxine	Sodium (2S)-2-(4-hydroxy-3-iodophenyl)propanoate	Thyroid hormone Subclass: Synthetic thyroxine	Hypothyroidism	Thyroid hormone receptor	Tablet (25 mcg, 50 mcg, 100 mcg, 200 mcg) Oral solution (100 mcg/mL)	Oral	Palpitations, weight loss, sweating	White to off-white crystalline powder	Freely soluble in water	pKa = 4.7	Phenol, iodine, ether
Metformin	1,1-Dimethylbiguanide	Antidiabetic Subclass: Biguanide	Type 2 diabetes mellitus	AMP-activated protein kinase (AMPK)	Tablet (500 mg, 850 mg, 1000 mg) Extended-release tablet (500 mg, 750 mg, 1000 mg)	Oral	Gastrointestinal upset, lactic acidosis	White crystalline powder	Soluble in water	pKa = 12.4	Biguanide
Insulin	Insulin (human)	Antidiabetic Subclass: Insulin	Diabetes mellitus	Insulin receptor	Injection (multiple formulations)	Subcutaneous	Hypoglycemia, weight gain, allergic reactions	Clear or cloudy solution	Soluble in water	N/A	Protein
Prednisone	6-alpha-methylprednisolone	Glucocorticoid Subclass: Corticosteroid	Inflammatory conditions, autoimmune diseases	Glucocorticoid receptor	Tablet (1 mg, 5 mg, 10 mg, 20 mg, 50 mg) Oral solution (5 mg/5 mL)	Oral	Osteoporosis, weight gain, hypertension	White crystalline powder	Freely soluble in water	pKa = 13.5	Ketone, alcohol, steroid
Estradiol	1,3,5(10)-estratriene-3,17-diol	Estrogen Subclass: Synthetic estrogen	Hormone replacement therapy, contraception	Estrogen receptor	Tablet (0.5 mg, 1 mg) Patch (various dosages)	Oral, transdermal	Nausea, headache, breast tenderness	White to off-white crystalline powder	Soluble in ethanol	pKa = 10.0	Phenol, alcohol, steroid
Glibenclamide	1-((4-(chlorobenzamido)phenyl)sulfonyl)-3-((4-methylphenyl)ethyl)urea	Antidiabetic Subclass: Sulfonylurea	Type 2 diabetes mellitus	Insulin receptor	Tablet (2.5 mg, 5 mg)	Oral	Hypoglycemia, weight gain	White crystalline powder	Soluble in water	pKa = 5.8	Sulfonylurea, amide
Sitagliptin	(3R)-3-amino-4-(trifluoromethyl)-1-[(3-hydroxy-1-oxo-2-azaspiro[4.5]dec-2-yl)methyl]piperidine-2-carbonitrile	Antidiabetic Subclass: DPP-4 inhibitor	Type 2 diabetes mellitus	Dipeptidyl peptidase-4 (DPP-4)	Tablet (25 mg, 50 mg, 100 mg)	Oral	Nausea, headache	White to off-white powder	Soluble in water	pKa = 9.3	Amines, nitriles
Rosiglitazone	(Z)-5-[4-(2-(4-(trifluoromethyl)phenyl)thiazol-2-yl)phenyl]methyl-2,4-thiazolidinedione	Antidiabetic Subclass: Thiazolidinedione	Type 2 diabetes mellitus	Peroxisome proliferator-activated receptor gamma (PPAR-γ)	Tablet (2 mg, 4 mg, 8 mg)	Oral	Edema, weight gain	White crystalline powder	Soluble in DMSO	pKa = 5.5	Thiazolidinedione
Liothyronine	3,3',5-triiodo-L-thyronine	Thyroid hormone Subclass: Synthetic T3	Hypothyroidism	Thyroid hormone receptor	Tablet (5 mcg, 25 mcg)	Oral	Palpitations, sweating	White to off-white powder	Freely soluble in water	pKa = 7.3	Iodine, phenol
Hydrocortisone	Pregn-4-ene-3,20-dione,21-hydroxy-	Glucocorticoid Subclass: Corticosteroid	Adrenal insufficiency, inflammatory conditions	Glucocorticoid receptor	Tablet (5 mg, 10 mg, 20 mg) Injection	Oral, IV	Osteoporosis, hypertension	White to off-white powder	Soluble in ethanol	pKa = 10.5	Ketone, alcohol, steroid
Desmopressin	1-Desamino-8-D-arginine vasopressin	Antidiuretic Subclass: Synthetic analog of vasopressin	Diabetes insipidus	Vasopressin receptor	Injection, nasal spray	Subcutaneous, intranasal	Headache, nausea	White powder	Soluble in water	pKa = 6.5	Amines
Somatropin	Recombinant human growth hormone	Growth hormone Subclass: Recombinant hormone	Growth hormone deficiency	Growth hormone receptor	Injection	Subcutaneous	Injection site reactions	White lyophilized powder	Soluble in water	N/A	Protein
Octreotide	Sandostatin	Antisecretory Subclass: Somatostatin analog	Acromegaly, carcinoid syndrome	Somatostatin receptor	Injection	Subcutaneous	Nausea, abdominal pain	White to off-white powder	Soluble in water	N/A	Peptide
Leuprolide	Leuprolide acetate	Gonadotropin-releasing hormone (GnRH) analog Subclass: Peptide	Prostate cancer, endometriosis	GnRH receptor	Injection	Subcutaneous	Hot flashes, weight gain	White powder	Soluble in water	N/A	Peptide
Fludrocortisone	21-Fluoropregn-4-ene-3,20-dione	Mineralocorticoid Subclass: Corticosteroid	Adrenal insufficiency	Mineralocorticoid receptor	Tablet (0.1 mg)	Oral	Hypertension, hypokalemia	White powder	Soluble in alcohol	pKa = 15.0	Ketone, alcohol, steroid
Levonorgestrel	(13S)-13-Ethyl-17-hydroxy-18-methyl-19-norpregna-4, 15-diene-3,20-dione	Progestin Subclass: Synthetic progestin	Contraception	Progesterone receptor	Tablet (0.75 mg, 1.5 mg)	Oral	Irregular menstrual bleeding	White to off-white powder	Soluble in ethanol	pKa = 10.4	Phenol, ketone, steroid
Clomiphene	Clomifene citrate	Estrogen receptor modulator Subclass: Selective estrogen receptor modulator (SERM)	Infertility	Estrogen receptor	Tablet (50 mg)	Oral	Hot flashes, multiple births	White powder	Soluble in ethanol	pKa = 8.0	Aromatics, ether
Dexamethasone	9-fluoro-11β,17-dihydroxy-16α-methyl-pregna-1,4-diene-3,20-dione	Glucocorticoid Subclass: Corticosteroid	Inflammation, allergies	Glucocorticoid receptor	Tablet (0.5 mg, 0.75 mg, 1 mg, 2 mg)	Oral	Osteoporosis, hypertension	White crystalline powder	Soluble in alcohol	pKa = 10.5	Ketone, alcohol, steroid
Calcitriol	1,25-Dihydroxycholecalciferol	Vitamin D analog Subclass: Active form of vitamin D	Hypoparathyroidism, rickets	Vitamin D receptor	Capsule (0.25 mcg, 0.5 mcg)	Oral	Hypercalcemia	Yellow to orange powder	Soluble in alcohol, oil	pKa = 7.4	Steroid

Drug Name

IUPAC Name

Classification (KD Tripathi)

Drug Application

Receptors

Dosage Form

Route of Administration

Adverse Reactions

Appearance

Solubility

pKa Value

Functional Groups

Levothyroxine

Sodium (2S)-2-(4-hydroxy-3-iodophenyl)propanoate

Thyroid hormone
Subclass: Synthetic thyroxine

Hypothyroidism

Thyroid hormone receptor

Tablet (25 mcg, 50 mcg, 100 mcg, 200 mcg)
Oral solution (100 mcg/mL)

Oral

Palpitations, weight loss, sweating

White to off-white crystalline powder

Freely soluble in water

pKa = 4.7

Phenol, iodine, ether

Metformin

1,1-Dimethylbiguanide

Antidiabetic
Subclass: Biguanide

Type 2 diabetes mellitus

AMP-activated protein kinase (AMPK)

Tablet (500 mg, 850 mg, 1000 mg)
Extended-release tablet (500 mg, 750 mg, 1000 mg)

Oral

Gastrointestinal upset, lactic acidosis

White crystalline powder

Soluble in water

pKa = 12.4

Biguanide

Insulin

Insulin (human)

Antidiabetic
Subclass: Insulin

Diabetes mellitus

Insulin receptor

Injection (multiple formulations)

Subcutaneous

Hypoglycemia, weight gain, allergic reactions

Clear or cloudy solution

Soluble in water

N/A

Protein

Prednisone

6-alpha-methylprednisolone

Glucocorticoid
Subclass: Corticosteroid

Inflammatory conditions, autoimmune diseases

Glucocorticoid receptor

Tablet (1 mg, 5 mg, 10 mg, 20 mg, 50 mg)
Oral solution (5 mg/5 mL)

Oral

Osteoporosis, weight gain, hypertension

White crystalline powder

Freely soluble in water

pKa = 13.5

Ketone, alcohol, steroid

Estradiol

1,3,5(10)-estratriene-3,17-diol

Estrogen
Subclass: Synthetic estrogen

Hormone replacement therapy, contraception

Estrogen receptor

Tablet (0.5 mg, 1 mg)
Patch (various dosages)

Oral, transdermal

Nausea, headache, breast tenderness

White to off-white crystalline powder

Soluble in ethanol

pKa = 10.0

Phenol, alcohol, steroid

Glibenclamide

1-((4-(chlorobenzamido)phenyl)sulfonyl)-3-((4-methylphenyl)ethyl)urea

Antidiabetic
Subclass: Sulfonylurea

Type 2 diabetes mellitus

Insulin receptor

Tablet (2.5 mg, 5 mg)

Oral

Hypoglycemia, weight gain

White crystalline powder

Soluble in water

pKa = 5.8

Sulfonylurea, amide

Sitagliptin

(3R)-3-amino-4-(trifluoromethyl)-1-[(3-hydroxy-1-oxo-2-azaspiro[4.5]dec-2-yl)methyl]piperidine-2-carbonitrile

Antidiabetic
Subclass: DPP-4 inhibitor

Type 2 diabetes mellitus

Dipeptidyl peptidase-4 (DPP-4)

Tablet (25 mg, 50 mg, 100 mg)

Oral

Nausea, headache

White to off-white powder

Soluble in water

pKa = 9.3

Amines, nitriles

Rosiglitazone

(Z)-5-[4-(2-(4-(trifluoromethyl)phenyl)thiazol-2-yl)phenyl]methyl-2,4-thiazolidinedione

Antidiabetic
Subclass: Thiazolidinedione

Type 2 diabetes mellitus

Peroxisome proliferator-activated receptor gamma (PPAR-γ)

Tablet (2 mg, 4 mg, 8 mg)

Oral

Edema, weight gain

White crystalline powder

Soluble in DMSO

pKa = 5.5

Thiazolidinedione

Liothyronine

3,3',5-triiodo-L-thyronine

Thyroid hormone
Subclass: Synthetic T3

Hypothyroidism

Thyroid hormone receptor

Tablet (5 mcg, 25 mcg)

Oral

Palpitations, sweating

White to off-white powder

Freely soluble in water

pKa = 7.3

Iodine, phenol

Hydrocortisone

Pregn-4-ene-3,20-dione,21-hydroxy-

Glucocorticoid
Subclass: Corticosteroid

Adrenal insufficiency, inflammatory conditions

Glucocorticoid receptor

Tablet (5 mg, 10 mg, 20 mg)
Injection

Oral, IV

Osteoporosis, hypertension

White to off-white powder

Soluble in ethanol

pKa = 10.5

Ketone, alcohol, steroid

Desmopressin

1-Desamino-8-D-arginine vasopressin

Antidiuretic
Subclass: Synthetic analog of vasopressin

Diabetes insipidus

Vasopressin receptor

Injection, nasal spray

Subcutaneous, intranasal

Headache, nausea

White powder

Soluble in water

pKa = 6.5

Amines

Somatropin

Recombinant human growth hormone

Growth hormone
Subclass: Recombinant hormone

Growth hormone deficiency

Growth hormone receptor

Injection

Subcutaneous

Injection site reactions

White lyophilized powder

Soluble in water

N/A

Protein

Octreotide

Sandostatin

Antisecretory
Subclass: Somatostatin analog

Acromegaly, carcinoid syndrome

Somatostatin receptor

Injection

Subcutaneous

Nausea, abdominal pain

White to off-white powder

Soluble in water

N/A

Peptide

Leuprolide

Leuprolide acetate

Gonadotropin-releasing hormone (GnRH) analog
Subclass: Peptide

Prostate cancer, endometriosis

GnRH receptor

Injection

Subcutaneous

Hot flashes, weight gain

White powder

Soluble in water

N/A

Peptide

Fludrocortisone

21-Fluoropregn-4-ene-3,20-dione

Mineralocorticoid
Subclass: Corticosteroid

Adrenal insufficiency

Mineralocorticoid receptor

Tablet (0.1 mg)

Oral

Hypertension, hypokalemia

White powder

Soluble in alcohol

pKa = 15.0

Ketone, alcohol, steroid

Levonorgestrel

(13S)-13-Ethyl-17-hydroxy-18-methyl-19-norpregna-4, 15-diene-3,20-dione

Progestin
Subclass: Synthetic progestin

Contraception

Progesterone receptor

Tablet (0.75 mg, 1.5 mg)

Oral

Irregular menstrual bleeding

White to off-white powder

Soluble in ethanol

pKa = 10.4

Phenol, ketone, steroid

Clomiphene

Clomifene citrate

Estrogen receptor modulator
Subclass: Selective estrogen receptor modulator (SERM)

Infertility

Estrogen receptor

Tablet (50 mg)

Oral

Hot flashes, multiple births

White powder

Soluble in ethanol

pKa = 8.0

Aromatics, ether

Dexamethasone

9-fluoro-11β,17-dihydroxy-16α-methyl-pregna-1,4-diene-3,20-dione

Glucocorticoid
Subclass: Corticosteroid

Inflammation, allergies

Glucocorticoid receptor

Tablet (0.5 mg, 0.75 mg, 1 mg, 2 mg)

Oral

Osteoporosis, hypertension

White crystalline powder

Soluble in alcohol

pKa = 10.5

Ketone, alcohol, steroid

Calcitriol

1,25-Dihydroxycholecalciferol

Vitamin D analog
Subclass: Active form of vitamin D

Hypoparathyroidism, rickets

Vitamin D receptor

Capsule (0.25 mcg, 0.5 mcg)

Oral

Hypercalcemia

Yellow to orange powder

Soluble in alcohol, oil

pKa = 7.4

Steroid

References

Tripathi, K. D. (2013). Essentials of Medical Pharmacology. 7th ed. New Delhi: Jaypee Brothers Medical Publishers.
Brunton, L. L., Hilal-Dandan, R., & Knollmann, B. C. (2017). Goodman & Gilman's: The Pharmacological Basis of Therapeutics. 13th ed. New York: McGraw-Hill Education.
DrugBank Online. (2021). Drug & Drug Target Database. [online] Available at: https://go.drugbank.com/ [Accessed 10 Sep. 2024].
National Center for Biotechnology Information. PubChem Database. [online] Available at: https://pubchem.ncbi.nlm.nih.gov/ [Accessed 10 Sep. 2024].
Stahl, S. M. (2013). Stahl's Essential Psychopharmacology: Neuroscientific Basis and Practical Applications. 4th ed. Cambridge: Cambridge University Press.