Medicinal Chemistry I

Medicinal Chemistry I is a core subject that explores the design, synthesis, and biological activity of drugs. It bridges organic chemistry and pharmacology to enhance understanding of therapeutic agents.

Key Highlights:

  • Studies drug classification, including antibiotics, sulfonamides, and chemotherapeutic agents.
  • Focuses on Structure-Activity Relationship (SAR) to relate chemical structure with drug action.
  • Explains mechanisms of action for various therapeutic compounds.
  • Covers drug synthesis and metabolic pathways.
  • Emphasizes physicochemical properties influencing drug absorption and efficacy.
  • Introduces principles of drug design and development.
  • Enhances skills needed for pharmaceutical research and formulation.
  • Builds a foundation for rational drug use and clinical application

Orphenadrine Citrate

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Orphenadrine Citrate treats muscle pain and stiffness, easing discomfort in acute musculoskeletal conditions. Orphenadrine Citrate is a centrally acting muscle relaxant with mild anticholinergic and analgesic effects. Chemical Formula: C₁₈H₂₃NO·C₆H₈O₇ Mechanism of Action of Orphenadrine Citrate: Anticholinergic + antihistaminic + NMDA antagonist Centrally acting skeletal muscle relaxant Therapeutic Uses of Orphenadrine Citrate: Muscle pain/spasm Parkinsonism … Read more

Methantheline Bromide

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Methantheline Bromide

Methantheline Bromide helps manage peptic ulcers by reducing gastric acid secretion. Methantheline Bromide is an anticholinergic agent with smooth muscle relaxant action. Chemical Formula: C₂₁H₂₆BrNO₃ Mechanism of Action of Methantheline Bromide: Non-selective muscarinic blocker Acts peripherally (no CNS effects) Therapeutic Uses of Methantheline Bromide: Peptic ulcers GI spasm (older drug, less common now) Side Effects: … Read more

Glycopyrrolate

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Glycopyrrolate

Glycopyrrolate reduces secretions, treats peptic ulcers, and aids in anesthesia premedication. Glycopyrrolate is an anticholinergic blocking muscarinic receptors with prolonged action. Chemical Formula: C₁₉H₂₈NO₃ Mechanism of Action of Glycopyrrolate: M3 antagonist (peripheral) → decreases secretions & GI motility Does NOT cross BBB Therapeutic Uses of Glycopyrrolate: Pre-op reduction of saliva and respiratory secretions Peptic ulcer … Read more

Dicyclomine Hydrochloride

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Chemical Formula: C₁₉H₃₅NO₂·HCl Mechanism of Action: Blocks M1 and M3 muscarinic receptors Also has direct antispasmodic action on GI smooth muscle Therapeutic Uses: Irritable bowel syndrome Functional GI disorders Abdominal cramps Side Effects: Drowsiness Dizziness Dry mouth Blurred vision Constipation CNS stimulation in high doses  SAR (Structure-Activity Relationship): Tertiary amine: Unlike quaternary analogs, it can … Read more

Clidinium Bromide

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Clidinium Bromide

Clidinium Bromide eases abdominal cramps and IBS symptoms by reducing gastric acid and spasms. Clidinium Bromide is an anticholinergic that blocks muscarinic receptors for GI relief. Chemical Formula: C₂₂H₂₆BrNO₃ Mechanism of Action of Clidinium Bromide: Antimuscarinic (M1 and M3) → reduces GI motility and secretions Does not cross BBB effectively Therapeutic Uses of Clidinium Bromide: … Read more

Cyclopentolate Hydrochloride

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Cyclopentolate Hydrochloride is used in ophthalmology for pupil dilation and cycloplegia. Cyclopentolate Hydrochloride is an anticholinergic blocking muscarinic receptors in the eye. Chemical Formula: C₁₇H₂₅NO₃·HCl Mechanism of Action of Cyclopentolate Hydrochloride: Muscarinic receptor blocker (M3 predominant) Shorter duration than atropine, longer than tropicamide Therapeutic Uses of Cyclopentolate Hydrochloride: Cycloplegic refraction in children Mydriasis for diagnostic … Read more

Tropicamide

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Tropicamide

Tropicamide is used in ophthalmology to dilate pupils for eye exams. Tropicamide acts as a short-acting anticholinergic mydriatic. Chemical Formula: C₁₇H₂₀N₂O₂ Mechanism of Action of Tropicamide: Selective muscarinic antagonist (M4/M3 > M1) Causes mydriasis (pupil dilation) and cycloplegia (paralysis of accommodation) Therapeutic Uses of Tropicamide: Ophthalmic exams (short-acting) Fundus examination Side Effects: Transient stinging Blurred … Read more

Ipratropium Bromide

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5. Ipratropium Bromide

Ipratropium Bromide is a short-acting anticholinergic bronchodilator with minimal systemic effects. Ipratropium Bromide treats asthma and COPD by relaxing airway muscles and easing breathing. Formula: C₂₀H₃₀BrNO₃ Mechanism: Blocks M3 receptors in bronchial smooth muscle → bronchodilation Minimal CNS effect (doesn’t cross BBB) Uses: COPD Asthma (adjunct) Side Effects: Dry mouth Cough Bitter taste Nasal dryness … Read more

Homatropine Hydrobromide

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Homatropine Hydrobromide

Homatropine Hydrobromide acts as an anticholinergic with shorter action than atropine. Homatropine Hydrobromide relieves eye disorders by dilating pupils and reducing spasms. Formula: C₁₆H₂₁NO₃·HBr Mechanism of Homatropine Hydrobromide: Muscarinic antagonist, shorter acting than atropine Uses of Homatropine Hydrobromide: Mydriasis Cycloplegia (eye exams) Side Effects: Transient stinging Increased intraocular pressure Dry mouth, photophobia

Scopolamine Hydrobromide

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Scopolamine Hydrobromide

Scopolamine Hydrobromide: Action – Blocks muscarinic receptors, reducing secretions, spasms, and vestibular stimulation. Scopolamine Hydrobromide: Uses – Anticholinergic drug for motion sickness, nausea, and pre-anesthetic medication. Formula: C₁₇H₂₁NO₄·HBr·3H₂O Mechanism of Scopolamine Hydrobromide: Muscarinic antagonist, stronger CNS penetration than atropine Uses of Scopolamine Hydrobromide: Motion sickness (transdermal) Postoperative nausea Sedation in palliative care Side Effects: Drowsiness … Read more

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