Antihistamine Flashcards
(56 cards)
1
Q
First Generation/Classical Antihistamines
A
- Aminoalkylethers/Ethanolamines
- Ethylenediamines
- Thiophene Derivatives
-Dibenzocycloheptenes - Alkylamines/Propylamine Derivatives
- Piperazine
- Phenothiazine
2
Q
Diphenhydramine, Bromodiphenhydramine, Dimenhydrinate, Doxylamine, Diphenylpyraline, Carbinoxamine
A
Aminoalkylethers/Ethanolamines
3
Q
Tripelennamine, Clestamine, Pyrilamine,
Mepyramine, Thonzylamine, Zolamine
A
Ethylenediamines
4
Q
Methapyrilene, Methaphenilene,
Thenyldiamine, Chlorothen
A
Thiophene Derivatives
5
Q
Cyproheptadine, Azatidine
A
Dibenzocycloheptenes
6
Q
Chlorpheniramine,
Pheniramine, Dexchlorpheniramine, Brompheniramine,
Dexbrompheniramine, Tripolidine, Phenylpropanolamine
A
Alkylamines/Propylamine Derivatives
7
Q
Cyclizine, Chlorcyclizine, Meclizine,
Buclizine
A
Piperazine
8
Q
Promethazine, Trimeprazine,
Methdilazine
A
Phenothiazine
9
Q
Second Generation Antihistamine
A
- Piperazine
- Piperidine
- Miscellaneous
10
Q
2nd Gen:
Cetirizine, Levocetirizine
A
Piperazine
11
Q
2nd Gen:
Loratadine, Desloratadine,
Fexofenadine
A
Piperidine
12
Q
2nd Gen:
Bilastine, Ebastine, Phenidamine,
Dimenthindene, Antazoline,
A
Miscellaneous
13
Q
- 2-benzhydryloxyethyldimethyl hydrochloride
A
Diphenhydramine
14
Q
- also used as night time sedative
- control of druh-induced parkinsonism
- in liquid form: control of coughs
A
Diphenhydramine
15
Q
- white, odorless, crystalline powder
- freely soluble in water, alcohol, chloroform
- available as “” maleate
with antiemetic and anticholinergic properties
A
Carbinoxamine
16
Q
- white crystalline powder
- water soluble
- 2[(4-bromophenyl)
phenylmethoxy)]-N, N-dimethylethanamine
A
Bromodiphenhydramine
17
Q
- aminoalkyl derivative
- white crystalline, colorless powder
- water soluble
- 8-
chlorotheophyllinate salt of diphenhydramine
A
Dimenhydrinate
18
Q
- piperidine derivative
- 4-
(diphenylmethoxy)-1-methylpiperidine - white crystalline powder
- soluble in water & alcohol
- insoluble in ether & benzene
- also posses: anticholinergic & sedative effects
A
Diphenylpyraline
19
Q
- white powder
- characteristic odor
- soluble in water & alcohol
- with sedative effects
- used with antitussives and decongestants for the relief of cough and cold
A
Doxylamine
20
Q
- alkyl ether derivative
- as “” fumerate
- white or slightly yellow crystalline powder
- slightly soluble in water & alcohol
- with anticholinergic and sedative effects
A
Clemastine
21
Q
these derivatives are highly effective H1 antagonists
- also exhibit high frequency CNS depression and GI side effects
A
Ethylenediamines
22
Q
- ethylenediamine derivative
- white crystalline powder
- characteristic odor
- soluble in water and alcohol
- occurs as maleate salt
- 2-[[2-
(dimethylamino) ethyl] (p-methoxybenzyl) amino] pyridine
maleate
A
Pyrilamine
23
Q
- ethylenediamine
- 2-[[2-
(dimethylamino) ethyl] 2-thenylamino]-pyridine - hydrochloride salt
- white crystalline powder
- water soluble
A
Methapyrilene
24
Q
- 2-((2-(dimethylamino)ethyl) (p-
methoxybenzyl)amino) pyrimidine - white crystalline powder
- water soluble
- used with Streptomycin in exudative human Tuberculosis
A
Thonzylamine
25
- is frequently employed in the treatment of perennial
and seasonal allergic rhinitis, allergic conjunctivitis due to
inhalant allergens and foods, simple allergic skim manifestations
of urticaria and angioedema, dermographism and anaphylactic
reactions as an adjunct to adrenaline.
Tripelennamine
26
can be prepared as follows : 2-
aminopyridine, prepared by the action of sodamide on pyridine,
is reacted with β-dimethylaminoethyl chloride in the presence
of sodamide, and the resulting 2-[2-(dimethylamino)
ethylamino] pyridine is subsequently condensed with benzyl
bromide in the presence of sodamide. The corresponding
hydrochloride salt is obtained from the base by treatment with
hydrogen chloride in an organic solvent
Tripelennamine
27
- all are chiral compounds
- most active H1 antagonists
- produce less sedation
- has significant anticholinergic activity
Propylamine Derivatives
28
- propylamine derivative
- dimethyl(3-phenyl-3-(2-pyridyl)propyl amine hydrogen
maleate
- white crystalline powder
- water soluble
- used widely in cough preparation
Pheniramine
29
- alkylamine derivative
- white crystalline powder
- water soluble
- has antimuscarinic activity
- causes moderate degree of sedation
Chlorpheniramine
30
- 3-(4-bromophenyl)-3-(2-pyridyl)
propyldimethylamine hydrogen maleate
- white crystalline powder
- water soluble
- with anticholinergic and sedative effects
- relief of hay fever and upper respiratory allergic systems
Brompheniramine
31
- pyrrolidine derivative
- white crystalline powder
- water soluble
- used with pseudoephedrine for tx of cough and common colds
Triprolidine
32
Possess tricyclic systems
Phenothiazine derivatives
33
- 10-(3-dimethylamino2-methyl propyl)-phenothiazine
- as tartarate salt
- more active than promethazine
- less active than chlorpromazine
- white crystalline powder
- odorless
- should be protected from light
- tx of pruritic symptoms due to urticaria
- tx of allergic and non allergic conditions
Trimeprazine
34
- 10-(2- dimethylaminopropyl) phenothiazine
- white colorless powder
- freely soluble in water
- soluble in alcohol and chloroform
- insoluble in ether and acetone
- store airtight container, protect from light
- has antimuscarinic, antiemetic and local anesthetic activity
Promethazine
35
- 10-(1-methyl-3-
pyrrolidinyl)methyl)phenothiazine
- light tan crystalline powder
- slight characteristic odor
- with sedative and local anesthetic properties
- tx of anaphylaxis
Methdilazine
36
- moderately potent derivative
- lower incidence of drowsiness
- defines as cyclic ethylenediamines
Piperazines
37
- piperazine derivative
- white crystalline powder
- slightly soluble in water, alcohol, and chloroform
- 1-(diphenylmethyl)-4-methyl piperazine
- given by mouth or parenterally to control post-operative and drug induced vomiting
Cyclizine
38
antihistaminic
activity of piperazines is reduced if ______ is introduced at 2 or
3 position of phenylring ring structures.
halogen
39
- 1-
(p-chlorobenzhydryl)- 4-methylpiperazine
Chlorcyclizine
40
- 1(p-chlorobenzhydryl)-4-(m-
methylbenzyl) piperazine
- white or slightly yellowish crystalline powder
- tasteless
- INSOLUBLE in water
- moderate antihistaminic activity
Meclizine
41
- piperazine derivative
- white or slightly yellow crystalline powder
- INSOLUBLE in water
- has antiemetic properties
Buclizine
42
- phenothiazine analogues
- sulfur atom of phenothiazine nucleus is replaced by an isosteric
vinyl group (—CH = CH— ) or a saturated ethyl bridge (—CH2—
CH2)
- A sp2 hybridized carbon atom replaces the nitrogen of
phenothiazine
Dibenzocycloheptenes
43
- H1 and Serotonin antagonist
- 4-
(5H-dibenzo[a,b]cyclohepten-5-ylidene)-1-methylpiperidine
- white to yellow crystalline powder
- odorless
- tx of migraine, anorexia, and diarrhea of carcinoid syndrome
Cyproheptadine
44
- white crystalline powder
- differs from cyproheptadine by having a pyridine ring instead of a benzene ring
- white crystalline powder
- water soluble
Azatadine
45
- miscellaneous antihistamines
- occur as tartarate salt
- odorless
- creamy white powder
- water soluble
- slightly acidic to litmus
Phenindamine
46
- white crystalline powder
- characteristic odor
- freely soluble in methanol and chloroform
- slightly soluble in water
- sensitive to light
- an indene derivative and occurs as maleate
Dimethindene
47
- imidazoline derivatives
- 2-[(N-benzylanilino) methyl]-2-imidazoline
- white crystalline powder
- bitter taste
- soluble in water
- occurs as phosphate salt
Antazoline
48
- 4 -tertiarybutyl 1-
4(4-diphenyl methoxy piperidine) butyrophenone
- potent, long acting antihistamine
- act against both early and late phase without any adverse effect on cardiovascular and CNS
- with anticholinergic effects
- active metabolite: carebastine
- low lipophilicity and greater molecular size
Ebastine
49
T or F
Injections of chlorpheniramine or promethazine are used as an
adjunct to adrenaline in the emergency treatment of
anaphylaxis and angioedema
T
50
is included as an anti-
emetic in a preparation for migraine.
Buclizine
51
bind only to peripheral
H1 receptors, and reduce allergic response with little or no
sedation. They have no central action, and are used only for
treatment of allergic reactions. These drugs have prolonged
antihistaminic effects and also binds to muscarinic, and
adrenergic receptors. These are divided into two chemical
classes.
2nd Generation Antihistamine
52
- inhibits cytochrome p450
- H2 histamine receptor antagonists
- inhibit basal as well as meal stimulated gastric secretion
Cimetidine
53
- 5-10 times more potent than cimetidine
- fewer side effects
- longer duration of action
- bind less to cytochrome p450
- H2 histamine receptor antagonists
Ranitidine
54
- more effective than ranitidine
- less than 45 percent of an oral dose is absorbed
- newer H2 histamine receptor antagonists
Famotidine
55
Overdose of antihistamines may cause what?
Involuntary movements
56
T or F
Side effects of antihistamines unclude GI problems and Hematologic reactions
T
