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Antihistamines (Lichtman) Flashcards

1
Q

What are 2 things histamines can be used to diagnose?

A
  1. Gastric acid secretion

2. Asthma

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2
Q

What receptors do antihistamines target in the stomach to control GERD?

A

H2

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3
Q

The antihistamine cromolyn sodium targets what and is it used acutely or prophylactically?

A
  1. Targets mast cells inhibiting their degranulation. 2. Only used prophylactically due to increased uptake time
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4
Q

What 2 reactions are histamines involved in?

A
  1. Inflammatory

2. Anaphylactic

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5
Q

What is the triple effect of histamine?

A
  1. Swelling
  2. Redness
  3. Edema
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6
Q

How is histamine synthesized?

A

Decarboxylation of amino acid L-histidine

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7
Q

I histamine is a bronchodilator or bronchoconstrictor?

A

A bronchoconstrictor

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8
Q

Histamine in nasal mucosa causes what?

A

Runny Nose

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9
Q

What are 3 conditions causing histamine release?

A
  1. Tissue injury
  2. Allergic reaction
  3. Drugs/foreign compounds
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10
Q

What is the term for exposure of an antigen to a previously sensitized (exposed) subject, associated with IgE antibodies?

A

Allergic reactions

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11
Q

Do antihistamines block all autocoids or just histamines at their receptor?

A

Only block at the receptor

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12
Q

What are 4 systems that histamine affects?

A
  1. Cardiovascular
  2. Smooth muscle of bronchiole
  3. Exocrine glands
  4. Peripheral nervous system
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13
Q

Is the histamine effect on the cardiovascular system, given subcutaneously or intramuscularly?

A
  1. Redden at injection site (vasodilation)
  2. Wheal/disk of edema w/in 1-2 min
  3. Large bright crimson flare or halo around wheal
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14
Q

Describe cardiovascular effects seen when Histamine is given intravenously.

A
  1. Fall in BP
  2. Cutaneous flush of face and trunk
  3. Increased skin temperature Intense headache
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15
Q

What does histamine do to nonvascular smooth muscle?

A

Contracts (bronchoconstriction)

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16
Q

What does histamine do to exocrine glands?

A
  1. increase gastric secretion (HCl and Pepsin)
  2. Increase salivary and lacrimal secretions (large dose)
  3. Increase catecholamine (epinephrine, norepinephrine) secretion from chromaffin cells of adrenal medulla
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17
Q

What are the peripheral nervous system symptoms associated with histamine?

A

Itching and pain

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18
Q

What are 6 glands whose secretions are increased by histamine?

A
  1. Gastric
  2. Salivary
  3. Sweat
  4. Pancreas
  5. Bronchial
  6. Lacrimal
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19
Q

What are 3 effects of histamine on arterioles, capillaries, and venules (triple effect associated)?

A
  1. Vasodilation
  2. Increase permeability (edema)
  3. Systemic hypotension
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20
Q

Where are 3 places where histamine increases vascular smooth muscle contraction?

A
  1. Bronchial tree
  2. Gastrointestinal tree
  3. Uterus
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21
Q

1 mg Histamine given subcutaneously serves what purpose?

A

Stimulates gastric secretion, which can be sampled and acid content determined

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22
Q

Does the 1mg histamine administration to determine gastric secretion have a major effect on blood vessels (vasodilation, increased permeability, systemic hypotension)?

A

No

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23
Q

Dry powder inhaler of histamine serves what purpose?

A

Assess pulmonary function

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24
Q

What are 6 toxic reactions and side effects of histamine?

A
  1. Cutaneous flushing
  2. Hypotension
  3. Headache
  4. Visual disturbances
  5. Dyspnea
  6. GI disturbances
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25
Q

What are 4 types of histamine receptors?

A

H1, H2, H3, H4

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26
Q

All histamine receptors are what type?

A

G-coupled protein receptors

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27
Q

Which histamine receptor mediates effects on smooth muscle leading to vasodilation, increased vascular permeability, and contraction of nonvascular smooth muscle?

A

H1 receptors

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28
Q

Which histamine receptor mediates histamine stimulation of gastric acid secretion?

A

H2 receptors

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29
Q

Which histamine receptor is a feedback inhibitor in CNS, gastrointestinal tract, lung, heart?

A

H3 receptors

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30
Q

Which histamine receptor mediates immune and inflammatory responses?

A

H4

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31
Q

Which 2 histamine receptors currently have no therapeutic agents against?

A

H3 and H4

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32
Q

What type of receptor antagonists are antihistamines?

A

Elective receptor antagonists

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33
Q

What are 3 general mechanisms of action for antihistamines?

A
  1. Block action of histamine at receptor
  2. Competes with histamine for binding
  3. Displaces histamine from receptor
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34
Q

When are antihistamines most beneficial?

A

when given early

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35
Q

What are 2 things antihistamines do cardiovascularly?

A
  1. Prevent dilation

2. Prevent increased permeability

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36
Q

Does HISTAMINE increase or decrease blood pressure?

A

Decreases blood pressure (vasodilation)

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37
Q

All H1 and H2 antagonists (antihistamines) are competitive or non-competitive antagonists?

A

Competitive (means they can be overcome by more agonist)

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38
Q

What does antihistamine do to exocrine secretions?

A

Decrease salivary, gastric, lacrimal and bronchial secretions (think xerostomia)

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39
Q

What does antihistamine do to immune response, e.g. an allergic reaction triggered by IgE?

A

Binds to receptors to prevent histamine from eliciting response

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40
Q

What is the mechanism of Action of HISTAMINE at H1 receptor?

A

Attaches to H1, G-coupled protein response leads to IP3 creation, causing a relases of stored Ca++

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41
Q

Antihistamine at the H1 receptor results in the a decrease of what AND where by inhibiting the production of IP3?

A

Decrease in Ca++ INSIDE of cell

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42
Q

What is the difference between an antihistamine and a decongestant with respect to side effects?

A

There are no rebound effects with antihistamine use

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43
Q

What do H1 blockers do for allergic rhinitis?

A

Relieve rhinorrhea, sneezing, itching of eyes and nose

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44
Q

What do H1 blockers do for the common cold and what other drugs are they paired with?

A

Dry out nasal mucosa. Paired with a nasal decongestant and analgesic.

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45
Q

What do H1 blockers do for allergic dermatoses?

A

Control itching associated with insect bite

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46
Q

What is an H1 blocker that can be used for preanesthetic sedation, prevention of nausea and vomiting, and also inhibits salivary and bronchial secretions, also can be used as a local anesthetic?

A

Phenergan/Promethazine

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47
Q

Promethazine/Phenergan, Bendectin, doxylamine with pyridoxine are H1 blockers that are used as antiemitics (prevent or treat nausea and vomiting) how?

A

Effects on muscarinic receptors

48
Q

Why is an H1 blocker used for parkinson’s disease?

A

It helps reduce tremors and muscle rigidity

49
Q

An H1 blocker can be used for what type of headaches?

A

Migraines

50
Q

What are 8 therapeutic uses of H1 blockers?

A
  1. Allergic rhinitis
  2. Common cold
  3. Allergic dermatoses
  4. Preanesthetic sedation
  5. Nausea and vomiting
  6. Hypnotics
  7. Parkinson’s disease symptoms
  8. Migraines
51
Q

What are the non-selective effects of H1 blockers (non-selective effects are associated with Gen-1 H1 blockers)?

A
  1. Antinausea and antiemetic effects
  2. Anti-parkinsonism effects
  3. Local anesthesia via Na+ channel blockers
52
Q

The antinausea, antiemetic, and antiparkinsonism non-selective effects of H1 blockers are due to their effects on what receptors?

A

Muscarinic

53
Q

Which gen 1 H1 blockers have non-selective effects that cause local anesthesia via sodium channel block?

A

Diphenhydramine

Promethazine/phenergan

54
Q

What is the characteristic of 2nd Gens H1 blockers that make them more selective than 1st Gen H1 blockers?

A

Do not cross blood brain barrier easily

55
Q

What are 3 second-generation H1 blockers that are more selective than first-generation H1 blockers?

A

Fexofenadine (Allegra)
Loratadine (Claritin)
Cetirizine (Zyrtec)

56
Q

Of the 3 second-generation H1 blockers, which is listed as long acting?

A

Loratadine (Claritin)

57
Q

What are the general characteristics of First Generation Antihistamine?

A
  1. Sedating side effects
  2. Anticholinergic side effects
  3. Many OTC (56% allergy pts use OTC antihistamine)
  4. Many inexpensive
58
Q

What are the general characteristics of First Generation Antihistamines?

A
  1. Sedating side effects
  2. Anticholinergic side effects
  3. Many OTC (56% allergy pts use OTC antihistamine)
  4. Many inexpensive
59
Q

What are the general characteristics of second-generation antihistamine?

A
  1. Not as sedating and drying as Gen 1 H1 blockers
  2. Do not cross BBB as easily as Gen 1
  3. Lipophobic
  4. Large Molecular size
  5. Electrostatic charge
60
Q

Which antihistamine seems to be the standard first-generation H1 blocker, that along with the normal anti-inflammatory, anti-itch, anti-rhinitis, vasodilation/permeability/itch blocking, also is
anti-muscarinic, gives pronounced sedation making it
useful as a hypnotic, and as a topical in Caladryl?

A

Diphenhyrdramine (benedryl)

61
Q

What are two first-generation blockers that have the standard
antihistamine characteristics, but are not as sedating as Diphenhydramine(Benedryl)?

A
  1. Chlorpheniramine (Chlor-trimeton)

2. Brompheniramine (Dimatane)

62
Q

Would a second-generation H1 blocker’s characteristic be sedation? Why or why not?

A

No, because they do not cross the blood-brain barrier readily

63
Q

Which second-generation H1 blocker has P-450 metabolism, and what other drug will affects its levels?

A

Loratidine (Claritin). Levels affected by anti-fungal agents.

64
Q

What is a first-generation H1 blocker that is anti-emetic via
antimuscarinic effects, blocks vasodilation/permeability,gives marked sedation, and can give local anesthesia via sodium channel blockade?

A

Promethazine (Phergan)

65
Q

Which first-generation H1 blocker is solely an antiemetic via
antimuscarinic effects, which also has the sedation and sodium channel blockade but does not block vasodilation and/or permeability?

A

Dimenhydrinate (Dramamine)

66
Q

Fexofenadine (allegra) a second-generation H1 blocker is a safe metabolite of what previous H1 blocker that caused
fatal heartbeat irregularities?

A

Safe metabolite of Terfenadine (Seldane)

67
Q

What first-generation H1 blocker is a metabolite of Hydroxyzine and has a potential for sedation?

A

Cetirizine (Zyrtec)

68
Q

What are 7 toxic reactions and side effects of H1 blockers?

A
  1. CNS depression (1st gen)
  2. Allergic rxn on topical application
  3. GI/appetite loss, nausea, vomiting
  4. Irritable, tachycardia, xerostomia, constipation
  5. Hallucinations, tremors
  6. Cross placenta
  7. Secreted in breast milk
69
Q

What is a concern if you take an H1 blocker and a barbiturate, opiate, general anesthetic or alcohol?

A

Potentiates CNS depression

70
Q

What is a risk associated with prescribing an H1
blocker that has antimuscarinic effects
(diphenhydramine[benedryl], promethazine[phergan], dimenhydrinate [Dramamine]) to a patient already on an
antimuscarinic drug?

A

Excessive blockade, e.g. dry mouth, constipation, blurred vision

71
Q

If Terfenadine (Seldane), no longer available, was taken with grapefruit juice, erythromycin, or other drugs that inhibit CYP3A4, what is the danger?

A

Cardiotoxicity

72
Q

Where are H2 receptors located?

A

Stomach

73
Q

What causes the release of histamine in the stomach and from what cells is it released?

A

Gastrin causes histamine release by enterochromaffin cells in the gastric mucosa

74
Q

Histamine released by entrochromaffin cells of the gastric mucosa in response to Gastrin, act on what cells to cause what?

A

Binds H2 receptors on parietal cells to cause HCl secretion

75
Q

What are 4 H2 blockers?

A
  1. Cimetidine (Tagmet)
  2. Ranitidine (Zantac)
  3. Famotidine (Pepcid)
  4. Nizatidine (Axid)
76
Q

Which H2 antagonist is associated with most side effects?

A

Cimetidine (Tagment)

77
Q

Are H2 antagonists competitive or non-competitive antagonists?

A

Competitive

78
Q

Do H2 antagonists have many affects beyond those on the gastric mucosa?

A

No

79
Q

What is a concern when taking H2 antagonists?

A

Increase stomach pH so it could affect the absorption of other drugs

80
Q

What are the 8 most common adverse effects associated with H2 antagonists?

A
  1. Diarrhea
  2. Dizziness
  3. Somnolence (drowsiness)
  4. Headache
  5. Rash
  6. Constipation
  7. Vomiting
  8. Arthralgia (joint pain)
81
Q

Are H2 antagonists ant-acids?

A

No, they do not buffer acid already released, they decrease output of subsequent HCl

82
Q

What are 7 H2 antagonist therapeutic uses?

A
  1. Duodenal ulcer
  2. Gastric ulcer
  3. Zolling-Ellison syndrome
  4. Gastroesophageal reflux disease (GERDs)
  5. GI obstruction pre-surgery
  6. Reflux esophagitis
  7. Antacid
83
Q

Why would an H2 antagonist not be used for Gastric ulcer much anymore?

A

Gastric ulcers are caused by H. pylori, so they are better treated by antibiotics

84
Q

What is a rare disorder that causes ulcers in the stomach and duodenum from excessive gastric pepsin and HCl,
treated with an H2 antagonist?

A

Zollinger-Ellison syndrome

85
Q

Why give a patient an H2 antagonist prior to surgery for gastric obstruction?

A

To elevate gastric pH by decreasing HCl secretion

86
Q

When an H2 antagonist is being used as an antacid,is it really acting as an antacid?

A

No, it is a pre-emptive way of decreasing acid release and increase stomach pH

87
Q

How do H2 antagonists work?

A

Displace Histamine from H2 receptor, turning of g-coupled protein increase of cAMP, which results in a decrease of Ca++

88
Q

What is the difference in H1 and H2 antagonist blocking of G-coupled protein when both result in a final decrease in Ca ++?

A

H1 cause a decrease in Ca++ by decreasing IP3

H2 cause a decrease in Ca++ by decreasing cAMP

89
Q

What are some CNS effects seen with the H2 antagonist Cimetedine(Tagment), and what population are they most common in?

A

Slurred speech, delirium, confusion in older patients or those with liver or kidney impairment

90
Q

The H2 antagonist Cimetedine (Tagmet) has minor and reversible effects on what endocrine function?

A

Antiandrogen effect: loss of libido, impotence, reduced sperm count

91
Q

The H2 antagonist Cimetedine (Tagment) can have what adverse effect on the liver?

A

Reversible cholestasis (impaired bile flow)

92
Q

How do H2 antagonists increase bioavailability of ethanol?

A

They block gastric alcohol dehydrogenase enzyme

93
Q

What is the only H2 antagonist that does not increase the bioavailability of ethanol?

A

Famotidine (Pepcid)

94
Q

Which H2 antagonist has the most drug interactions because it affects the cytochrome P450 pathway and reduces blood flow through the liver?

A

Cimetidine (Tagmet)

95
Q

Agents that inhibit gastric secretion can be expected to have what type of drug interaction?

A

Alter bioavailabilty and rate of absorption of many other drugs

96
Q

What substance serves as an inhibitor of Histamine release, other granular contents and leukotriene production?

A

Cromolyn sodium

97
Q

Does Cromolyn sodium (Intal, Nasalcrom) have bronchodilating capability?

A

No

98
Q

What is the method of action of Cromolyn sodium (Intal, Nasalcrom)?

A

It inhibits pulmonary mast cell degranulation in response to stimuli (e.g. cell bound IgE and antigen interation)

99
Q

Does Cromolyn sodium (Intal, Nasalcrom) relax bronchial or other smooth muscle?

A

No

100
Q

What is the benefit of long term administration of Cromolyn sodium (Intal, Nasalcrom)?

A

Diminishes bronchial hyperactivity

101
Q

Is Cromolyn sodium (Intal, Nasalcrom) effective for acute asthma attack?

A

No

102
Q

Cromolyn sodium (Intal, Nasalcrom) reduces the need for what other mild to moderate asthma treatment?

A

Reduce the need for steroid or bronchodilators

103
Q

What are other therapeutic uses for Cromolyn sodium (Intal, Nasalcrom) beyond mild to moderate asthma prophylaxis?

A
  1. Allergic rhinitis
  2. Atopic diseases of the eye
  3. Giant papillary conjunctivitis
104
Q

How long does it take for Cromolyn sodium (Intal, Nasalcrom) to become effective?

A

2-3 weeks

105
Q

Cromolyn sodium (Nasalcrom) is used to treat what?

A

Allergic rhinitis as a nasal spray

106
Q

Cromolyn sodium (Intal) is used to treat what?

A

Asthma as an aerosol powder and solution

107
Q

Cromolyn sodium (Opticrom) is used to treat what?

A

Allergic conjunctivitis

108
Q

What are some side effects of Cromolyn sodium?

A

Irritation from powder inhaler, stinging, burning, bad taste, cough, sneeze, allergic reaction

109
Q

How do antihistamines produce their effect?

A

Competition at the receptor

110
Q

Is sedation a side effect of histamine?

A

No

111
Q

What are 3 antihistamines that are approved for use by heavy-machine operators because they do not have a sedative effect?

A
  1. Fexofenadine (Allegra)
  2. Certirazine (Zyrtec)
  3. Loratadine (Claritin)
112
Q

Are antihistamines ever given to someone to reverse anaphylaxis?

A

No. Anaphylaxis is acute. Its reversal agent is epinephrine.

113
Q

What is the most common sign of histamine?

A

Triple effect

114
Q

A low does of what substance can be used to diagnose asthma when inhaled?

A

Histamine

115
Q

H2 Blockers do what?

A

Decrease HCl

xD3 Pharm Exam 1 (4 decks)

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