Centrally Acting Agents

Centrally acting agents are drugs that influence the central nervous system, altering brain or spinal cord function to produce therapeutic or behavioral effects. They act by crossing the blood-brain barrier and modifying neurotransmitter release, receptor activation, or neuronal excitability, often through agonist, antagonist, or reuptake mechanisms. In pharmacology, these agents include analgesics, sedatives, anesthetics, antidepressants, antipsychotics, and drugs for neurological disorders. Studying their pharmacokinetics, receptor selectivity, and effects on neural circuits helps researchers understand therapeutic benefits, adverse effects, drug interactions, and strategies for developing safer treatments.

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JoVE Core - Pharmacology

Centrally Acting Muscle Relaxants: Therapeutic Uses

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2023

Centrally acting muscle relaxants reduce muscle tone and tension by interfering with the postsynaptic reflexes in the central nervous system. Centrally acting drugs are classified into spasmolytic and antispasmodic drugs. Spasmolytic drugs such as baclofen, diazepam, and tizanidine inhibit spinal motor neurons and decrease muscle tone. Spasmolytic drugs are administered for severe and chronic spasms due to multiple sclerosis, cerebral palsy, stroke, and spinal cord and muscle injuries. However,...

Adrenergic Agonists: Direct-Acting Agents

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2023

Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine. These agents can be classified...

Adrenergic Agonists: Indirect-Acting Agents

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2023

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors. One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...

Peripherally and Centrally Acting Muscle Relaxants: A Comparison

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2023

Skeletal muscle relaxants can target the central nervous system [CNS] to reduce muscle tension or act directly at the neuromuscular junction to induce temporary paralysis. These two classes of muscle relaxants are called centrally acting muscle relaxants and peripherally acting muscle relaxants. They differ in their action, mechanism, administration route, and clinical uses. Centrally acting muscle relaxants can be further divided into spasmolytic and antispasmodic drugs. Spasmolytic drugs,...

Forces Acting on Chromosomes

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2021

During mitosis, chromosome movements occur through the interplay of multiple piconewton level forces. In prometaphase, these forces help in chromosome assembly or congression at the equatorial plane, eventually leading to their alignment at the metaphase plate. The forces acting on the chromosomes are space and time-dependent; therefore, they vary with the position of the chromosomes as the cell progresses through mitosis. Microtubules and motor proteins exert two types of forces on...

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