Kaur: Derm IE 2

What 1st gen AH subclass also effects the other receptors such as cholienrgic, adrenergic, dopaminergic, and serotonergic?

Ethylenediamines

T/F: Ethanolamines has a long half-life

F → short

Which 1st gen antihistamines sub class has decreased sedation compared to Ethanolamines and Ethylenediamines?

Alkylamines

Which 1st gen antihistamines sub class have a long duration of action?

Alkylamines

What is the acid metabolite of hydroxyzine?

Cetirizine

Cetrizine is formed from _ of the terminal _ alcohol to the corresponding _

Oxidation

Primary

Carboxylic acid

T/F: Cetirizine is usually classified with the 1st generation sedating antihistamines

F → 2nd-gen non-sedating antihistamines

How do Loratadine and Desloratadine not accumulate in the CNS?

Efflux proteins

2nd Gen H1 Antihistamines

T/F: Improved H1 selectivity

T/F: Has sedative qualities

T/F: Little structure variety

T/F: More anticholnergic activity

T/F: Long half-life

T. Improved H1 selectivity

F. Little or no sedative qualities

F. Wide structure variety

F. Less anticholinergic activity

T Long half-life

Histamine mainly exists as what at physiologic pH?

Monocation

What structure in diphenylhydramine helps with decreased sedative effects?

Chlorotheophyllinate salt

T/F: A-adrenergic receptor agonists (Catecholamines) have high oral bioavailability and slow metabolism

F → Poor oral bioavailability, rapid metabolism

The pharmacophore for a- adrenergic agonists (phenylethanolamine agonists) consists of

• Substituted bezene

• Aliphatic amine separated from benzene by two carbons

• R- hydroxyl at C1 carbon (R configuration gives maximum direct activity)

T/F

• Phenylethanolamine agonists have poor oral activity

• Phenylethanolamine agonists have a racemic mixture

• Phenylethanolamine agonists have a natural product

• Phenylethanolamine agonists are widely used as eye drops

F. Good oral activity

T

T

F. Nasal decongestants

What structure slows down metabolism in phenylethanolamine? Via?

Methyl position at 2

By MAO

_ sites have a wider range of substitutent tolerance in phenylethanolamines

Alpha

How do a1-agonists (phenylethanolamines) become selective?

If phenyl substitution is only a 3’-OH → activity is reduced

Which phenylethanolamines have a longer duration of action? Why?

Metaraminol, Methoxamine

Bc/ they’re not a substrate for COMT or MAO

Which functional groups on a-agonist molecules keep them out of the CNS?

Phenolic hydroxy groups

What FGs are helpful in water solubility?

Charged hydrochloride salt and hydroxyl group

T/F: Ethylenediamines are sedative

T

Which drug class are used as OTC sleep aids?

Ethanolamines

T/F: Catecholamines are non-selective

T

Which catecholamines are most associated with the following structure:

1. R=H

2. R=CH3

1. R=H

   1. Noradrenaline/Norepinephrine/Arterenol

2. R=CH3

   1. Adrenaline/Epinephrine