Term
|
Definition
-potent A and B1 receptor agonist
-substrate for MAO and COMT
-parenteral administration
-used as a pressor
-sodium bisulfite used in preparations to prevent oxidation |
|
|
Term
|
Definition
-potent A, B1 and B2 receptor agonist
-substrate for MAO and COMT
-parenteral administration
-sodium bisulfite used in preparations to prevent oxidation
-available as many salts: hydrochloride, nitrate, bitartrate
-uses: anaphylaxis, glaucoma, in combination with local anesthetics |
|
|
Term
|
Definition
-potent A1 receptor agonist
-substrate for MAO
-administration: parenteral, oral, local
-uses: mydriasis without cycloplegia, glaucoma, pressor, nasal decongestant |
|
|
Term
| Naphazoline, Tetrahydrozoline, Oxymetazoline |
|
Definition
-partial agonists at A receptor
-administered locally/topically to promote vasoconstriction
-basic nature of imidazoline ring causes compounds to exist in ionized form at physiologic pH
-uses: nasal and ophthalmic decongestants |
|
|
Term
|
Definition
-(phenylimino)imidazolidine
-selective for A2 receptor agonist
-the basicity of the guanidine group (pka=13.6) is decreased (to pka=8.0) because of the attachment of the dichlorophenyl ring
-clinical effect linked to activation of A2 receptors in the nucleus of the solitary tract (cardiovascular center)
-administration: oral, parenteral, transdermal
-uses: hypertension, opiate withdrawal |
|
|
Term
|
Definition
-A2 receptor agonist
-"open-ring" imidazolidines
-two atom bridge to the guanidine group decreases the pKa so that the drug is mostly non-ionized at physiological pH
-guanbenz has the shortest t-1/2 at ~6 hours. half-life of clonidine and guanfacine is 12-16 hours
-administration: oral
-uses: hypertension |
|
|
Term
|
Definition
-methyldopa- a prodrug metabolized to active A2 receptor agonist (1R,2S)-A-methylnorephinephrine
-act at CNS A2 receptors to decrease sympathetic outflow
-water soluble, ester hydrochloride salt Methyldopate is used in parenteral solutions
-administration: methyldopa, oral; methyldopate, parenteral
-uses: hypertension |
|
|
Term
|
Definition
-A2 receptor agonist
-use: glaucoma |
|
|
Term
|
Definition
-A2 receptor agonist
-use: muscle spasticity |
|
|
Term
|
Definition
-non-selective B receptor agonist
-bronchodilation
-increased cardiac output
-metabolized by conjugation reactions (phase II) and by COMT
-not sensitive to MAO
-administration: oral, parenteral, local (inhaled)
-uses: asthma, COPD, cardiostimulant |
|
|
Term
| Metaproterenol, Terbutaline |
|
Definition
-resorcinol derivatives
-selective B2 receptor agonists
-bronchodilation
-cardiac effects observed only at high doses
-not metabolized by MAO or COMT
-longer duration of action than isoproterenol
-administration: oral, parenteral, local (inhaled)
-uses: asthma, COPD; Terbutaline used as a tocolytic (prevent premature labor) |
|
|
Term
|
Definition
-Meta hydroxymethyl derivatives
-selective B2 receptor agonists
-bronchodilation
-cardiac effects observed only at high doses
-not metabolized by MAO or COMT
-longer duration of action than isproterenol
-administration: oral, local (inhaled)
-uses: asthma, COPD |
|
|
Term
|
Definition
-selective B2 receptor agonist
-bronchodilation
-not metabolized by MAO or COMT
-onset of action: salmeterol 10-20min, formoterol <5 min
-longer duration of action
-administration: inhaled (metered-dose inhaler and powder)
-uses: long-term asthma, COPD
- not recommended for acute treatment of asthma symptoms |
|
|
Term
|
Definition
-selective B2 receptor agonist
-administration: oral, parenteral
-uses: tocolytic |
|
|
Term
|
Definition
-B1 receptor agonist
-dopamine derivative
-available as a racemic mixture
-(+)enantiomer: potent B1 receptor agonist
-(-)enantiomer: potent A1 receptor agonist, potency for B receptors reduced 10x
-net effect is positive inotropic effect on heart with little chronotropic effect
-metabolized by COMT and conjugation, not sensitive to MAO
-short half life (~2min)
-administered: parenteral
-use: acute heart failure, shock |
|
|
