Hormones Part 1 | Medicinal Chemistry | Dr. Aqsa Murtaza

    

PHARMA BY AQSA MURTAZA (PharmD)

Aim to help Pharmacy Students. We cover a wide range of topics, from Medicinal Chemistry, Pharmacology, and Drug Interactions to Medication Management and Disease State Management.

MEDICINAL CHEMISTRY

HORMONES

• Oxytocin
• Vasopressin
• Estrogen
• Progesterone
• Cortisol
• Glucagon
• Insulin
• Testosterone
• Aldosterone

 

HORMONES

• The endocrine system is made up of the endocrine glands that secrete hormones.
• Chemical messenger
• Work slowly, over time, and controls many functions in our body.
• Hormones are carried by the blood throughout the entire body and affect specific cells.
• Metabolism, growth, etc.

 

 

OXYTOCIN

Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2

• “Quick Birth”
• Induce labor
• Has 9-Amino acids, bound with a disulfide bridge
• Molecular formula = C43H66N12O12S2
• Release from Posterior Pituitary Gland
• Given parenterally.

ADR

• Severe uterine contraction
• Water retention
• Nasal irritation

CONTRAINDICATION

• Uterine rupture
• Smooth muscle contraction 

INTERACTION

• Anesthetics like Cyclopropane and Halothane → Uterine rupture

 

VASOPRESSIN

Cys-Tyr-Phe-Glu-Asn-Cys-Pro-Arg-Gly-NH2

• Enhances memory (Smart drug)
• Antidiuretic hormone
• Release from Posterior Pituitary Gland
• Molecular Formula = C46H65N15O12S2

INDICATION

• Antidiuretic agent → decreases urine excretion
• Vasoconstrictor agent → increase blood pressure
• Diabetes insipidus

ADR

• Sweating
• Diarrhea
• Abdominal pain
• Palpitation

CONTRAINDICATION

• Asthma
• Epilepsy

DRUG INTERACTIONS

• Cimetidine → Inhibit the effect of vasopressin
• Lithium → Vasopressin effects increases
• Alcohol, Heparin, Norepinephrine → Vasopressin effect inhibited

 

ESTROGEN

USES/RELEASE OF OVULATION 

• During ovulation
• Pregnancy
• Used as contraceptive

PROPERTIES

• White crystalline powder
• IV, SC route of administration
• Water insoluble and soluble in benzyl benzoate
• Available in 3 forms:

1. Estriol
2. Estradiol
3. Estrone

• Management of menopausal symptoms
• Replacement therapy in hormone deficiency

 MECHANISM OF ACTION

Bind to sex hormone binding globulin and produces effect by protein synthesis.

ADR

• Fluid retention
• Infertility in males
• Nausea

CONTRAINDICATION

• Children

SAR

• The Hydroxyl group in the aromatic ring is important for its activity, replacement leads to a decrease in drug activity.
• An aromatic ring with a hydroxyl group is also very important.
• Alkylation of the aromatic ring decreases the activity.
• Unsaturation of ring B decreases the activity.

 

PROGESTERONE

INDICATION

• Use in combination with estrogen
• Lower uterine contraction

PROPERTIES

• Odorless, white to off-white color crystalline powder
• Water insoluble
• Solubilize in organic solvents
• Available in suppositories
• Available in 2 forms

1. Progesterone
2. 17 Alphahydroxy Progesterone

• Secreted by the corpus luteum in females and by the testes in males.
• Synthesized also by the adrenal cortex in both males and females

ACTION 

• Reduces uterine contraction
• Use in hormonal replacement therapy

ADR

• Insomnia
• GI Upset
• Fluid retention
• Mental disturbances
• Acne
• Nausea and Vomiting

SAR

• Unsaturation of ring B or C increases the activity.
• Substitution with the halogen group in ring B increases the activity of te drug.
• The steroidal nucleus is essential for its activity.
• The Methyl group is important for its activity replacement as it leads to the deactivation of the drug.

INTERACTION

• Phenytoin, Rifampicin, and Phenobarbital lead to therapeutic failure.

 

THANK YOU

Dr. Aqsa Murtaza