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PHA6115 > [PHA6115 lec] Endocrine Drugs > Flashcards

[PHA6115 lec] Endocrine Drugs Flashcards

1
Q

Composed of several hormone-releasing organs

A

Endocrine System

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2
Q

How does the endocrine system maintain body functions and homeostasis?

A

By releasing hormones which are used for several body functions (e.g., growth, reproduction, and defense)

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3
Q

Endocrine drugs work like __________?

A

Hormones (Natural, Semi-synthetic or Synthetic)

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4
Q

Classification of Endocrine Drugs based on Structure

A
  1. Peptide (majority)
  2. Steroidal (adrenal cortex / sex hormones) –> CCPT backbone
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5
Q

Classification of Endocrine Drugs based on Function

A
  1. Releasing hormones
  2. Stimulating hormones
  3. Thyroid and pancreatic, adrenal hormones
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6
Q

Complex disease characterized by uncontrolled glucose homeostasis associated with several minor and major complications

A

Diabetes

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7
Q

3 Cardinal Signs of Diabetes

A
  1. Polyuria
  2. Polyphagia
  3. Polydipsia
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8
Q

[Type of DM]
Insulin-dependent, juvenile onset, require insulin therapy for their lifetime

A

DM Type 1

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9
Q

[Type of DM]
Insulin-independent, adult onset (commonly), may or may not have insulin therapy

A

DM Type 2

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10
Q

[Type of DM]
Glucose intolerance during pregnancy

A

Gestational Diabetes

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11
Q

[Type of DM]
Results for non-usual causes or from other diseases present in the patient that may not concern insulin levels

A

Secondary DM

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12
Q

[Diabetes]
Therapy is directed at maintaining _________?

A

Euglycemic states (normal blood sugar)

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13
Q

It is a 51-amino acid protein with two chains linked by a disulfide bond

A

Insulin

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14
Q

Where is insulin produced?

A

Beta cells of pancreas

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15
Q

MOA of Insulin

A

Transports glucose into adipose and muscle cells via GLUT 4

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16
Q

SAR of Insulin

A

N- and C- terminals of the AA Chain A and B are essential for insulin receptor binding

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17
Q

Insulin is produced via __________ of proinsulin

A

Proteolytic modifications

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18
Q

Proinsulin is formed by removing what from preproinsulin?

A

24-amino acid

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19
Q

[Classification and Pharmacokinetics of Insulin Preparation]
Examples of Rapid-acting

A

Lispro, Aspart, Glulisine (LiAsGlu)

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20
Q

[Classification and Pharmacokinetics of Insulin Preparation]
Examples of Short-acting

A

Human Insulin - regular

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21
Q

[Classification and Pharmacokinetics of Insulin Preparation]
Examples of Intermediate-acting

A

Lente, NPH insuline (isophane)
> NPH means Neutral Protamine Hagedorn

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22
Q

[Classification and Pharmacokinetics of Insulin Preparation]
Examples of Long-acting

A

Ultralente, Glargine, Detemir (UltraDeGlar)

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23
Q

Agents that stimulate the release of insulin from the beta cells of the pancreas

A

Insulin secretagogues

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24
Q

2 Pharmacophores of Insulin Secretagogues

A
  1. Sulfonylurea
  2. Meglitinides
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25
Q

MOA of Sulfonylureas

A

Binds to SUR1 at K-channel and opens the voltage-gated Ca-Channel = Increased intracellular CA and exocytotic release of insulin

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26
Q

SAR of Sulfonylureas

A

1st generation
- small lipophilic at R1
- alkyl/cyclic substituent at R2
- high dose, long plasma half-life, short DOA, high chance for ADR

2nd generation
- large meglitinide group at R1
- high potency, low dose, rapid onset, short plasma half-life, long DOA

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27
Q

1st generation Sulfonylureas

A

Tolbutamide, Chlorpropramide, Acetohexamide (CAT-amide)

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28
Q

2nd generation Sulfonylureas

A

Glyburide or Glibenclamide, Glipizide, Glimepiride (“Gly or gli”)

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29
Q

MOA of Meglitinides

A

Similar to sulfonylureas; Repaglinide binds also to SUR1, SUR2A, and SUR2B = Extrapancreatic effects

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30
Q

SAR of Meglitinides

A

Meglitinide is a prototype structure - a benzoic acid derivative of the non-sulfonylurea moiety of Glibenclamide or Glyburide

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31
Q

Examples under Meglitinides

A

Repaglinide
- rapid onset, short DOA
- doesn’t cause prolonged hyperinsulinemia
- available in the market

Nateglinde
- rapid onset, longer DOA

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32
Q

Anti-diabetic agent that is considered the 1st line treatment with lifestyle change

A

Biguanides

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33
Q

T or F: Biguanides are highly distributed and excreted unchanged in urine

A

True

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34
Q

MOA of Biguanides

A
  • decreases gluconeogenesis
  • increases glycogenolysis and glycolysis
  • increases insulin sensitivity
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35
Q

SAR of Biguanides

A

2-linked guanidine moiety (Bi + guanidie)

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36
Q

Insulin Sensitizers / PPAR Agonists, what does PPAR mean?

A

Peroxisome Proliferator Activated Receptor

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37
Q

MOA of Insulin Sensitizers or PPAR Agonists

A
  • PPAR controls gene expression, increases glucose transporter expression = Increased insulin sensitivity of the body
  • Slows down gluconeogenesis and lower systematic fatty acids
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38
Q

SAR of Insulin Sensitizers or PPAR Agonist

A

Thiazolidinedione pharmacophore

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39
Q

For agonist activity of the Thiazolidinedione pharmacophore, R must be __________?

A

Para- substituted phenyl ring attached via methylene bridge

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40
Q

Examples of Insulin Sensitizers or PPAR Agonists

A

Pioglitazone
- only available in the market

Troglitazone
- not used due to severe hepatotoxicity

Rosiglitazone
- limited availability due to increase cardiovascular effects

(TroPioRosi “-glitazone”)

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41
Q

Enzyme that is made of maltase, sucrase, isomerase, and glucomylase found in the small intestine

A

Alpha-glucosidase

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42
Q

MOA of A-Glucosidase Inhibitors

A

Inhibits a-glucosidase to inhibit carbohydrate breakdown = Preventing absorption of mono/disaccharides

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43
Q

SAR of A-Glucosidase Inhibitors

A

Mimic the natural substrates of a-glucosidase by having similar structures

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44
Q

This group aids in mimicking natural disaccharide substrate

A

Polyhydroxy groups

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45
Q

Examples of A-Glucosidase Inhibitors

A

Acarbose
- extremely low oral bioavailability

Voglibose
- poolry absorbed

Miglitol
- absorbed orally, not metabolized = excreted unchanged

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46
Q

30-31 amino acid peptide produced by prohormone convertase enzymes from proglucagon

A

GLP-1

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47
Q

MOA of GLP-1 Agonist

A

GLP-1 is released in response to food = Promotes insulin secretion from pancreas

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48
Q

SAR of GLP-1 Agonist

A

GLP-1 Agonist analogs have penultimate amino acid modification to resist metabolism by DPP-IV

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49
Q

[GLP-1 Agonist Agents’ Modification]
Penultimate Ala –> Gly

A

Exenatide

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50
Q

[GLP-1 Agonist Agents’ Modification]
Lys26 has a-glutamoyl-(N-a-hexadaconyl) and Lys34 is replaced by Arg34

A

Liraglutide

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51
Q

[GLP-1 Agonist Agents’ Modification]
Fusion of 2 modified GLP-1 to albumin

A

Albiglutide

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52
Q

[GLP-1 Agonist Agents’ Modification]
Fusion of 2 modified N-terminal GLP-1 analog to IgG4 Fc domain

A

Dulaglutide

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53
Q

Alternatives to GLP-1 Agonist Analogs

A

DPP-IV Inhibitors

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54
Q

MOA of DPP-IV Inhibitors

A

Binds to active site in DPP-IV

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55
Q

SAR of DPP-IV Inhibitors

A

3 pharmacophore structure:
a-aminoacylpyrrolidine, xanthine, pyrimidine-2,4-dione

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56
Q

Group that binds to the active serine site in DPP-IV

A

Cyano group

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57
Q

T or F: DPP-IV Inhibitors can be taken alone or with metformin or thiazolidinedione

A

True

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58
Q

Examples of DPP-IV Inhibitors

A

Saxagliptin and Vildagliptin (a-aminoacylpyrrolidine)

Sitagliptin
- piperazine fused pyrazole with a-aminoacyl moiety

Alogliptin
- pyrimidine-2,4-dione pharmacophore

Linagliptin
- xanthine pharmacophore

(VildaSaSiAloLi “-gliptin”)

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59
Q

37-amino acid hormone released with insulin

A

Amylin

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60
Q

MOA of Amylin Agonist

A

Suppress glucagon secretion and delay gastric emptying time = Modulation of appetite centers to maintain glucose plasma level

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61
Q

SAR of Amylin Agonist

A

Pramlintide
- more water soluble
- reduced aggregation

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62
Q

Aids in reabsorption of glucose from renal proximal tubules

A

SGLT2

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63
Q

MOA of SGLT2 Inhibitor

A

Inhibit SGLT2 = Decreased renal threshold for glucose = Increased urinary glucose excretion

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64
Q

SAR of SGLT2 Inhibitor

A

Phlorizin pharmacophore and a glucose moiety that bind to Thr156 and Lys 157 moiety of transporter

65
Q

T or F: SGLT2 Inhibitor is recommended from patients with DM Type 1 and patients with renal impairment

A

False, not recommended

66
Q

Examples of SGLT 2 Inhibitors

A

Phlorizin
- pharmacophore with glucose

Dapagliflozin, Empagliflozin, Canagliflozin

(Phlorizin + CanaDapaEmpa “-gliflozin”)

67
Q

Only mammalian organ that can incorporate iodine into organic molecule

A

Thyroid gland

68
Q

Source of throxine (T4) and triiodothyronine (T3)

A

Thyroid gland

69
Q

Medications for disorders associated to thyroid gland

A

HRT and/or anti-thyroid drugs

70
Q

Major regulatory step in Thyroid Glands

A

TSH release

71
Q

Stimulates thyroid gland to create thyroid hormon

A

TSH

72
Q

T3 or T4: Which one is the precursor?

A

T4 - thyroxine

73
Q

T3 or T4: Which is the active form and is a negative feedback molecule for the anterior pituitary?

A

T3 - triiodothyronine

74
Q

3 Types of Thyroid Replacement Hormones

A
  1. Hypothalamic - TRH
  2. Pituitary - TSH
  3. Organ - T4 and T3
75
Q

Examples of Anti-thyroid Drugs

A

Thioamides, Anions, Radioactive I2, Propranolol

76
Q

MOA of T4 and T3

A

T4 is transported into the cells and is converted into T3

T3 then enters the nucleus, interacts with DNA = Stimulation/Inhibition of gene transcription

77
Q

SAR of T4 and T3

A

2 phenyl rings linked with X group

78
Q

[SAR of T4 and T3]
X is

A

Oxygen

79
Q

[SAR of T4 and T3]
R1 and R4’

A

R1 - alanine group
R4’ - OH group

80
Q

[SAR of T4 and T3]
R3, R5, R3’

A

Iodine (T3)

81
Q

[SAR of T4 and T3]
R5’

A

Iodine (T4)

82
Q

[SAR of T4 and T3]
Potency between L and D-isomers

A

L-isomer is more potent than D-isomer

83
Q

Slower-acting than iodides

A

Thioamides

84
Q

MOA of Thioamides

A

Potent inhibitors of thyroperoxidase (TPO)

85
Q

SAR of Thioamides

A

Thiouracil C2 keto/enol and unsubstituted N1 - essential for activity

Thiouracil C4 keto and C5/C6 alkyl substitution - increased activity

N1 methyl of MMI = Removes inhibition of peripheral deiodination

86
Q

Examples of Thioamides

A

Propylthiouracil (PTU) and Methimazole (MMI)

87
Q

MOA of Anions

A

Competitively blocks iodide transporter = Blocks iodine uptake

88
Q

Examples of Anions

A

Pertechnetate, Perchlorate, Thiocyanate

89
Q

MOA of Radioactive I2

A

Destroys thyroid gland cells = Lowers hormone levels

90
Q

MOA of Propranolol

A

Inhibits deiodination of T4 to T3

91
Q

Unsaturated steroid alcohol derived from terpenoid squalene

A

Sterols

92
Q

What backbone does sterols possess?

A

CPPP

93
Q

Where are sterols derived?

A

Natural sources such as;
Cholesterol (animals)
Phytosterol (plants)
Ergosterol (fungi)

94
Q

What are the functions of sterols?

A
  1. Regulates cell membrane fluidity
  2. Precursor for bile acids
95
Q

T or F: Sterols are also precursors for steroid hormones

A

True
Glucocorticoids, Mineralocorticoids, Sex hormones

96
Q

General Steroid MOA

A

Bind to steroid receptors which are kept inactive by HSP

97
Q

General Steroid MOA

A

Bind to steroid receptors which are kept inactive by HSP

Steroid-receptor enters nucleus several process occurs with Co-A and HRE of DNA

Steroid effects are seen in transcription of mRNA and translation of proteins

98
Q

[Adrenal Glands and Different Zones]
Outermost

A

Glomerulosa - mineralocorticoids - Na and fluid reabsorption, K excretion

99
Q

[Adrenal Glands and Different Zones]
Middle

A

Fasciculata - glucocorticoids - Intermediary metabolism, CV function, growth, immunity

100
Q

[Adrenal Glands and Different Zones]
Innermost

A

Reticularis - gonadal hormones - primary and secondary sex characteristics, reproduction

101
Q

Examples of Steroidal Drugs

A

Aldosterone (mineralcorticoid)

Cortisol (glucocorticoid)

Estradiol
- primary estrogen
- 2ndary female characteristics

Testosterone
- primary androgen
- 2ndary male characteristics

Progesterone
- primary progestin
- prepares uterus for pregnancy

102
Q

T or F: Steroid structures will always contain CPPP backbone, like a modified cholesterol molecule

A

True

103
Q

11-hydroxylated steroid hormone

A

Glucocorticoids

104
Q

17-hydroxylated steroid hormone

A

Sex hormones

105
Q

Only aldehyde-containing steroid hormone

A

Aldosterone

106
Q

Only aromatic steroid hormone

A

Estrogen

107
Q

SAR of Steroidal Drugs

A

C20 thiofluoromethyl = Increases GC receptor affinity

21-OH required for MC activity

21-Cl increases GC receptor affinity

107
Q

SAR of Steroidal Drugs

A

C20 thiofluoromethyl = Increases GC receptor affinity

21-OH required for MC activity

21-Cl increases GC receptor affinity

X16 (a/b-methyl) substitution = Decreases MC activity but increases GC activity

6a/9a halogenation (F/Cl) = Enhances activity for both GC and MC

3-keto and delta-4,5 = Essential for activity of both GC and MC

11-b = Essential for GC activity

Delta-1,2 = Increases GC activity

108
Q

Mainly used for their anti-inflammatory activity but can also be used for non-inflammatory uses

A

Glucocorticoids

109
Q

MOA of Glucocorticoids

A

Promotes histone deacetylase activity = Reverse action of histone acetyltransferase = Inhibition of gene expression for inflammation

110
Q

Uses of Glucocorticoids

A

Gout, arthritis, SLE, colitis, asthma, hypoglycemia, Addison’s disease

111
Q

Availability of Glucocorticoids

A

Systemic and Topical corticosteroids

112
Q

Examples of Glucocorticoids

A

Hydrocortisone
- aka cortisol

Prednisolone

113
Q

[Non-inflammatory Effects of Glucocorticoids]
CNS

A

Profound behavioral changes when given in large doses

114
Q

[Non-inflammatory Effects of Glucocorticoids]
Excretory

A

Normal renal excretion (MC effect)

115
Q

[Non-inflammatory Effects of Glucocorticoids]
Gastric

A

Stimulation of gastric acid secretion, which can lead to
development of peptic ulcer

116
Q

[Non-inflammatory Effects of Glucocorticoids]
Bone

A

Antagonism of the effect of vitamin D on calcium absorption

117
Q

[Non-inflammatory Effects of Glucocorticoids]
Blood

A

Increase of platelets and RBC

118
Q

[Non-inflammatory Effects of Glucocorticoids]
Respiratory

A

Development of fetal lung

119
Q

Uses of Mineralocorticoids

A

Addison’s disease, diagnosis of Conn’s syndrome

120
Q

Examples of Mineralocorticoids

A

Aldosterone
- regulation of salt and water in the body
- not commercially available

Fludrocortisone
- used to raise cortisol and for detecting Conn’s syndrome through the fludrocortisone suppression test

121
Q

AKA male sex hormones produced by the Leydig cells of testis, adrenal, and ovary

A

Androgens

122
Q

Major androgen in males that is synthesized from progesterone or dehydroepiandrosterone (DHEA)

A

Testosterone

123
Q

Testosterone is activated by ___________ into dihydrotestosterone (DHT) that occurs usually in the prostate organ of the body

A

5a-reductase

124
Q

Effects of Androgen

A

Normal development of male during infancy to puberty

Development of facial, pubic, and auxiliary hair; darkening of skin

Anabolic action

Increased muscle size and strength

Increased RBC production

Helps maintain normal bone density

124
Q

Effects of Androgen

A

Normal development of male during infancy to puberty

Development of facial, pubic, and auxiliary hair; darkening of skin

Anabolic action

Increased muscle size and strength

Increased RBC production

Helps maintain normal bone density

125
Q

[Anti-androgen agents]
Androgen-receptor blockers

A

Spironolactone

126
Q

[Anti-androgen agents]
Examples of Spironolactone

A

Flutamide, Nilutamide, Trifluorophenyl derivatives

127
Q

[Anti-androgen agents]
Agents for BPH or Prostate Cancer

A

Finasteride and Dutasteride
- steroid amide as 5a-reductase inhibitor

Quinazolines
- alpha-1 blockers

Abiraterone
- steroidal agent that blocks enzymes responsible for the synthesis of androgens

Serenoa repens
- Saw palmetto

128
Q

C-18 steroid with aromatic ring

A

Estrogen

129
Q

Estrogen exists in 3 forms

A

Estradiol (most potent)
Estrone
Estriol

130
Q

C21 with 3-keto-4-ene, C20 keto)

A

Progestins

131
Q

Progestins naturally occur as _______

A

Progesterone (most potent)

132
Q

Uses of Estrogen and Progestins

A

Hypogonadism in young females, contraception, and HRT

133
Q

Aside from sex characteristics, Estrogen contributes to ________

A

Bone integrity - prevents bone resorption

134
Q

MOA of Estrogens

A

Binds to ER(a/b) = Dimerization - migrates to the cell nucleus and binds to specific estrogen-response elements (ERE) = DNA transcription

135
Q

ADRs of Estrogen

A

Increased risk for breast and endometrial cancer, breast tenderness

Nausea, increased risk for migraine

HTN

Thromboembolic events

136
Q

Progestins added to estrogen during HRT to reduce unwanted effects

A

Modified Progestins

137
Q

SAR of Modified Progestins

A

Androstane or pregnane steroid nuclei = Essential for progestic activity

Etc

138
Q

MOA of Anti-Progestins

A

Competes with progesterone at receptor sites

139
Q

SAR of Anti-Progestins

A

Contain C11-phenyl group that aids in competitive receptor blockade

140
Q

Examples of Anti-Progestins

A

Ulipristal
- for emergency contraception

Mifepristone
- for abortion

141
Q

[Anti-Estrogen for Cancer Therapy]
Used for estrogen-related cancer

A

Aromatase Inhibitor

Ex. Anastrozole, Exemestane

142
Q

[Anti-Estrogen for Cancer Therapy]
Used for breast CA, but may cause endometrial CA

A

Selective Estrogen Receptor Modulators (SERMs)

Ex. Ospemifene - dyspareunia
Raloxifene - osteoporosis
Clomifine - infertility

143
Q

3 Primary Hormones involved in managing Ca levels in the Body

A

Calcitonin (CT), Parathyroid hormone (PTH), and Vitamin D

144
Q

Promotes urinary secretion of Ca and prevents intestinal absorption during hyperglycemia

A

Calcitonin

145
Q

Promotes inhibits renal secretion of Ca and promotes bone resorption during hyperglycemia

A

PTH

146
Q

MOA of 2nd Generation SERMs

A

Agonist activity on estrogen receptors in osteoblast and osteoclast but in the breast and uterus

147
Q

SAR of 2nd Generation SERMs

A

Triarlyethylene derivatives of Tamoxifen

Phenol/Phenoxy ring system = Essential to mimic A-ring of estrogen for receptor binding

Propeller orientation of 3 rings = Essential for receptor binding and activity

148
Q

Examples of 2nd Generation SERMs

A

Lasofoxifene, Ospemifene, Bazedoxifene, Toremifene

149
Q

MOA of Bisphophonates

A

Binds to the hydroxyapatite of the bone = Prevents osteoclast activity = Reduces osteoclast proliferation and life span

150
Q

SAR of Bisphophonates

A

Analogs of pyrophsphates

R1-OH = Maximizes affinity for hydroxyapatite = Improved antiresorptive activity

R2 substitution can vary

Amino alkyl with 3-atom chain with the N atom in a heterocyclic ring = Optimal activity

151
Q

Examples of Bisphophonates

A

Etidronate, Risedronate, Alendronate, Pamidronate

(RiEtiAlePami “-dronate”)

152
Q

[Other agents]
Decrease bone resorption by osteoclast

A

Calcitonin

153
Q

[Other agents]
PTH analog, increases number of osteoblast

A

Teriparatide

154
Q

[Other agents]
Calcimimetic, increase Ca sensitivty = Lower PTH secretion = Lower serum Ca levels

A

Cinacalcet

155
Q

[Other agents]
Increases mineralization of hydroxyapatite = Stronger bones/teeth

A

Sodium fluoride

156
Q

[Other agents]
Increase bone formation and decrease bone resorption

A

Strontium ranelate

PHA6115 (2 decks)

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