Peripherally selective drug
Peripherally selective drugs have their primary mechanism of action outside of the central nervous system, 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
- 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 – 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
- 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 – an adrenergic receptor agonist
- Peptides
- 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