Girish Mahajan (Editor)

Peripherally selective drug

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Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood-brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opiates cause sedation when given at a sufficiently high dose, but peripherally selective opiates can act on the rest of the body without entering the brain and are less likely to cause sedation.

Examples

  • α-Methylserotonin – a serotonin receptor agonist
  • Alvimopan – a μ-opioid receptor antagonist used in the treatment of postoperative ileus
  • Atenolol – a beta blocker
  • Benserazide – an aromatic L-amino acid decarboxylase inhibitor used in combination with levodopa in the treatment of Parkinson's disease
  • Bethanechol – a muscarinic acetylcholine receptor agonist used in the treatment of dry mouth and urinary retention
  • Bisoprolol – a beta blocker
  • Carbachol – a non-selective acetylcholine receptor agonist used in the treatment of glaucoma
  • Carbidopa – an aromatic L-amino acid decarboxylase inhibitor used in combination with levodopa in the treatment of Parkinson's disease
  • Cetirizine – a non-sedating antihistamine
  • Darolutamide – an antiandrogen used in the treatment of prostate cancer
  • Domperidone – a D2 receptor antagonist used as an antiemetic, gastroprokinetic agent, and galactogogue
  • Dopamine – a dopamine receptor agonist used as a cardiac stimulant and positive inotropic agent
  • Eluxadoline – a μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist used in the treatment of diarrhea-predominant irritable bowel syndrome
  • Epinephrine (adrenaline) – an adrenergic receptor agonist used as a cardiac stimulant and in the treatment of anaphylaxis
  • Fenoldopam – a D1 receptor agonist used as an antihypertensive agent
  • Fexofenadine – a non-sedating antihistamine
  • Fulvestrant – an antiestrogen used in the treatment of breast cancer
  • GABA – a dietary supplement
  • Glycopyrronium bromide – an anticholinergic
  • Hyoscine butylbromide – an anticholinergic
  • Itopride – a D2 receptor antagonist and acetylcholinesterase inhibitor used as a gastroprokinetic agent
  • Labetalol – a beta blocker
  • Loperamide – a μ-opioid receptor agonist used as an antidiarrheal
  • Loratadine – a non-sedating antihistamine
  • Methacholine – a choline ester and muscarinic acetylcholine receptor agonist
  • Methylhomatropine – an anticholinergic
  • Methylnaltrexone – a μ-opioid receptor antagonist used in the treatment of opioid-induced constipation
  • Midodrine – an α1-adrenergic receptor agonist used in the treatment of orthostatic hypotension
  • Nadolol – a beta blocker
  • Naloxegol – a μ-opioid receptor antagonist used in the treatment of opioid-induced constipation
  • Norepinephrine (noradrenaline) – an adrenergic receptor agonist
  • Peptides (e.g., insulin, oxytocin, vasopressin, opioid peptides, many others)
  • Pirenzepine – an anticholinergic
  • Pyridostigmine – an acetylcholinesterase inhibitor and parasympathomimetic
  • Serotonin – a serotonin receptor agonist
  • Sotalol – a beta blocker
  • Timepidium bromide – an anticholinergic
  • Trimetaphan camsilate – a nicotinic acetylcholine receptor antagonist
  • Trospium chloride – an anticholinergic
  • References

    Peripherally selective drug Wikipedia