Peripherally selective drug

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.^[1]

Examples[]

α-Methylserotonin – a serotonin receptor agonist
Alvimopan – a μ-opioid receptor antagonist used in the treatment of postoperative ileus
Anastrozole – an aromatase inhibitor used in the treatment of breast cancer
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
Desloratadine – a non-sedating antihistamine
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
Levocetirizine – a non-sedating antihistamine
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
Metopimazine – a D₂ receptor antagonist used in the treatment of nausea, vomiting, and gastroparesis
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 and proteins (e.g., insulin, oxytocin, vasopressin, opioid peptides, growth factors, many others)
Pirenzepine – an anticholinergic
Pyridostigmine – an acetylcholinesterase inhibitor and parasympathomimetic
Serotonin – a serotonin receptor agonist
Sotalol – a beta blocker
Terfenadine – a non-sedating antihistamine
Timepidium bromide – an anticholinergic
Trimetaphan camsilate – a nicotinic acetylcholine receptor antagonist
Trospium chloride – an anticholinergic

References[]

^ Stein, C; Zöllner, C (2009). "Opioids and sensory nerves". Handbook of Experimental Pharmacology. 194 (194): 495–518. doi:10.1007/978-3-540-79090-7_14. ISBN 978-3-540-79089-1. PMID 19655116.

External links[]

Media related to Peripherally selective drugs at Wikimedia Commons

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[1] Stein, C; Zöllner, C (2009). "Opioids and sensory nerves". Handbook of Experimental Pharmacology. 194 (194): 495–518. doi:10.1007/978-3-540-79090-7_14. ISBN 978-3-540-79089-1. PMID 19655116.

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