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

Structure–Activity Relationship (SAR) of Anticonvulsants

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Structure–Activity Relationship (SAR) of Anticonvulsants

Structure–Activity Relationship (SAR) of Anticonvulsants explains molecular features crucial for seizure control. Structure–Activity Relationship (SAR) of Anticonvulsants links chemical modifications to efficacy and safety. Anticonvulsants vary structurally but share key SAR features within their classes: Hydantoins (e.g., Phenytoin): Diphenyl groups on the hydantoin ring are crucial. Electron-withdrawing groups enhance potency. Hydrogen bonding supports sodium channel … Read more

Carbamazepine

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Carbamazepine

Carbamazepine treats epilepsy, trigeminal neuralgia, and bipolar disorder effectively It stabilizes neuronal membranes by blocking voltage-gated sodium channels. Formula: C₁₅H₁₂N₂O Mechanism of Carbamazepine: Na⁺ channel blocker → inhibits repetitive neuronal firing Also modulates glutamate release Uses of Carbamazepine: Focal & generalized tonic-clonic seizures Trigeminal neuralgia Bipolar disorder (mania) Side Effects: Diplopia, ataxia SIADH → hyponatremia … Read more

Phenacemide

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Phenacemide

Phenacemide is an anticonvulsant used in refractory epilepsy when other treatments fail. It stabilizes neuronal activity, reducing abnormal electrical discharges in the brain. Formula: C₉H₁₀N₂O₂ Mechanism of Phenacemide: Unclear; likely stabilizes neuronal membranes Possibly inhibits Na⁺ channels Uses of Phenacemide: Refractory epilepsy (no longer used) Side Effects: Severe toxicity: Aplastic anemia Liver damage Psychosis

Methsuximide

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Methsuximide

Methsuximide is prescribed for controlling absence seizures when other drugs are less effective. It reduces abnormal neuronal firing by blocking T-type calcium channels in the CNS. Chemical Formula: C₁₂H₁₅NO₂ Mechanism of Methsuximide : T-type Ca²⁺ channel blockade Therapeutic Uses of Methsuximide: Refractory absence seizures May be used when ethosuximide fails Side Effects: CNS effects: dizziness, … Read more

Phensuximide

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Phensuximide

Phensuximide treats absence seizures by controlling abnormal brain electrical activity. It reduces T-type calcium currents, stabilizing neuronal excitability in epilepsy. Chemical Formula: C₁₁H₁₃NO₂ Mechanism of Action: T-type calcium channel blocker Therapeutic Uses of Phensuximide: Absence seizures (older use) Side Effects of Phensuximide: Drowsiness GI upset Hepatic dysfunction Less effective than ethosuximide

Ethosuximide

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Ethosuximide

Ethosuximide is effective in treating absence seizures by reducing abnormal brain activity. It blocks T-type calcium channels in neurons, stabilizing electrical activity. Chemical Formula: C₇H₁₁NO₂ Mechanism of Action: Selectively inhibits T-type calcium channels Suppresses thalamic burst firing → prevents spike-wave discharges Therapeutic Uses: First-line agent for absence seizures Side Effects: GI upset (nausea, vomiting) Drowsiness … Read more

Paramethadione

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Paramethadione reduces neuronal excitability by blocking T-type calcium channels in the CNS. It is prescribed for absence seizures when other treatments are less effective. Chemical Formula: C₆H₁₁NO₂ Mechanism of Action: Same as trimethadione (T-type Ca²⁺ channel blocker) Therapeutic Uses of Paramethadione: Absence seizures (less effective than trimethadione) Side Effects of Paramethadione: Milder than trimethadione but … Read more

Trimethadione

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Trimethadione

Trimethadione is prescribed for absence seizures when other treatments are ineffective It stabilizes neuronal activity by reducing T-type calcium currents in the thalamus.. Chemical Formula: C₆H₁₁NO₂ Mechanism of Action: Blocks T-type Ca²⁺ channels in thalamic neurons Reduces thalamocortical rhythmicity (key in absence seizures) Therapeutic Uses of Trimethadione: Absence seizures (historical) Occasionally used in refractory cases … Read more

Ethotoin

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Ethotoin

Ethotoin is prescribed for the management of generalized tonic-clonic and partial seizures.  It stabilizes neuronal membranes by reducing repetitive firing, controlling epileptic activity. Chemical Formula: C₁₁H₁₆N₂O₂ Mechanism: Sodium channel blocker Less potent than phenytoin Therapeutic Uses of Ethotoin: Tonic-clonic seizures Partial seizures Side Effects of Ethotoin: Sedation GI upset Ataxia Less severe toxicity vs. phenytoin … Read more

Mephenytoin

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Chemical Structure of Mephenytoin

Mephenytoin stabilizes neuronal membranes by reducing repetitive firing through sodium channel blockade. It is an anticonvulsant used in managing generalized tonic-clonic and partial seizures. Chemical Formula: C₁₂H₁₄N₂O₂ Mechanism of Mephenytoin: Sodium channel blocker (like phenytoin) Rapid oral absorption Uses of Mephenytoin: Tonic-clonic and partial seizures (historical) Side Effects: Aplastic anemia (rare but serious) Drowsiness, ataxia … Read more