Serotonin histamine cology > Untitled Deck > Flashcards

Untitled Deck Flashcards

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1
Q

What are the key autacoids involved in physiological and pathological processes?

A
  • Histamine
  • Serotonin (5-HT)
  • Prostaglandins

They play vital roles in inflammation, allergy, neurotransmission, vascular tone regulation, and smooth muscle activity.

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2
Q

What are the pharmacological targets of histamines, serotonin, and prostaglandins?

A
  • Antihistamines
  • Serotonin agonists and antagonists
  • Prostaglandin analogues and leukotriene antagonists

These drug classes are used to manage diseases such as asthma, migraine, allergic reactions, and inflammation.

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3
Q

Histamine is produced from which amino acid?

A

Histidine

Histamine is stored in granules in mast cells, basophils, eosinophils, and histaminergic neurons.

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4
Q

What are the three receptors that histamines bind to?

A
  • H1 receptors
  • H2 receptors
  • H3 receptors

H1 and H2 receptors are excitatory, while H3 receptors are present on all types of tissues.

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5
Q

What are the physiological functions of H1 receptors?

A
  • Allergic and IgE-mediated anaphylaxis
  • Vasodilation
  • Increased capillary permeability
  • Gastrointestinal smooth muscle contractions
  • Itching and pain

H1 receptors play a significant role in immune response and allergic reactions.

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6
Q

What is the mechanism of action of H1 antihistamines?

A

Inverse agonism on H1 receptors

This mechanism blocks the effects of histamine at H1 receptors.

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7
Q

Name examples of H1 antihistamines.

A
  • Diphenhydramine
  • Doxylamine
  • Brompheniramine
  • Chlorpheniramine
  • Hydroxyzine
  • Cetirizine
  • Promethazine
  • Loratadine
  • Fexofenadine

These antihistamines vary in their sedative effects and clinical uses.

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8
Q

What are the common side effects of first-generation antihistamines?

A
  • Sedation
  • Dizziness
  • Nausea
  • Constipation
  • Dry mouth
  • Urinary retention

These side effects are more pronounced with first-generation antihistamines.

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9
Q

True or false: Second-generation antihistamines are primarily used for allergic rhinitis.

A

TRUE

Second-generation antihistamines are preferred due to fewer sedative effects.

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10
Q

What are the therapeutic uses of H2 receptor antagonists?

A
  • GERD
  • Upset stomach
  • Heartburn
  • GI ulcers
  • Stress-induced gastritis

H2RAs inhibit gastric acid secretion by blocking H2 receptors on parietal cells.

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11
Q

What is the precursor of serotonin?

A

Tryptophan

Tryptophan is converted to serotonin through hydroxylation and decarboxylation.

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12
Q

What are the subtypes of serotonin receptors?

A
  • 5HT1
  • 5HT2
  • 5HT3

Each subtype has different clinical significance and therapeutic targets.

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13
Q

What is the role of 5HT1a receptors?

A

Regulation of anxiety and mood

Agonists of these receptors are used in anxiety disorders and as antidepressants.

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14
Q

What is the mechanism of action of H2 receptor antagonists?

A

Competitive inhibitors of H2 receptors

They inhibit gastric acid secretion by blocking histamine’s action on parietal cells.

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15
Q

What are the main actions of bradykinin?

A
  • Pain
  • Vasodilation
  • Increased permeability

Bradykinin is part of the plasma kinin system and plays a role in inflammation.

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16
Q

What are the sources of prostaglandins?

A

Arachidonic acid (COX pathway)

Prostaglandins are involved in vasodilation, fever, and pain.

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17
Q

What is the clinical significance of serotonin 5HT2 receptors?

A

Involvement in psychosis

These receptors are targeted in the treatment of various psychiatric disorders.

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18
Q

What is the action of leukotrienes?

A
  • Chemotaxis (LTB₄)
  • Bronchoconstriction (LTC₄)

Leukotrienes are derived from arachidonic acid and play a role in inflammation and asthma.

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19
Q

What is the clinical use of 5HT1a receptors?

A
  • Regulation of anxiety
  • Regulation of mood

Complete agonist of presynaptic 5HT1a and partial agonist at postsynaptic 5HT1a.

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20
Q

What is Buspirone classified as?

A

5HT1a agonist

Used for anxiety disorders, antidepressant, anti-aggressive, and antiemetic.

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21
Q

What do 5HT1b/1d receptors involve?

A
  • Migraine
  • CNS
  • Vasoconstriction

Triptans are used for acute migraine attacks.

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22
Q

What is the role of 5HT2a receptors?

A
  • Regulate perception
  • Regulate cognition

5HT constricts smooth muscles of bronchi and GI.

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23
Q

What are the clinical uses of 5HT3 receptors?

A
  • Chemotherapy-induced nausea
  • Radiation therapy nausea
  • Gastrointestinal regulation

5HT3 regulates peristalsis movement.

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24
Q

What is the mechanism of action of triptans?

A

Activating 5HT1 receptors

Causes vascular constriction, first-line therapy for acute migraine attack.

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25
What are the **side effects** of triptans?
* Feeling of warmth * Dizziness * Tightness or heaviness in the chest * Chest pain (rare) ## Footnote Medication overuse headache can occur if taken more than 10 days per month.
26
What is **Trazodone** classified as?
* 5HT2A antagonist * Serotonin reuptake inhibitor (SARI) ## Footnote Involved in the regulation of mood and behavior.
27
What are the **5HT3 receptor antagonists**?
* Ondansetron * Granisetron * Palonosetron ## Footnote Used for nausea and vomiting in chemotherapy and surgery.
28
What is the clinical use of **Prucalopride**?
5HT4 agonist ## Footnote Classified as a prokinetic agent for treating constipation.
29
What are **eicosanoids** derived from?
Arachidonic acid ## Footnote Includes prostaglandins, thromboxane, prostacyclin, and leukotrienes.
30
What is the mechanism of action of **Misoprostol**?
* Inhibits HCl secretion * Increases mucus secretion * Increases bicarbonate ## Footnote Used for prevention of NSAID-induced GI ulcers.
31
What are the **therapeutic uses** of **Dinoprostone**?
* Abortifacient effects * Induce cervical ripening ## Footnote Classified as a PGE2 analog.
32
What are the **PGF2α analogs**?
* Latanoprost * Travoprost * Bimatoprost * Unoprostone ## Footnote Used for lowering intraocular pressure in open-angle glaucoma.
33
What is the role of **Prostacyclin (PGI2)**?
* Potent vasodilator * Inhibits platelet aggregation ## Footnote Used for pulmonary hypertension.
34
What do **leukotrienes** play a major role in?
* Bronchoconstriction * Increase permeability * Increase mucus secretion ## Footnote Produced from arachidonic acid by lipoxygenase.
35
What is **Montelukast** classified as?
Cysteinyl leukotriene receptor antagonist ## Footnote Used for asthma maintenance therapy and allergic rhinitis.
36
Leukotriene inhibitors used in children > 2yrs?
Montelukast ## Footnote Montelukast is commonly prescribed for asthma and allergic rhinitis.
37
What is the **PGF2a analog**?
1. PGF2a analog ## Footnote This refers to prostaglandin F2 alpha, which has various physiological effects.
38
What is an **Eicosanoid PGE1 analog**?
2. Eicosanoid PGE1 analog ## Footnote PGE1 is involved in vasodilation and inhibition of platelet aggregation.
39
What are the **precursors** for serotonin?
Tryptophan ## Footnote Tryptophan is an essential amino acid that serves as a precursor for serotonin synthesis.
40
What are the **precursors** for histamine?
Histidine ## Footnote Histidine is an amino acid that is converted into histamine by the enzyme histidine decarboxylase.
41
What are **LTC4 and LTD4**?
5. LTC4 and LTD4 ## Footnote These are leukotrienes involved in inflammatory responses and bronchoconstriction.
42
What is **N-acetyl-p-benzoquinoneimine**?
6. N-acetyl-p-benzoquinoneimine ## Footnote This is a toxic metabolite associated with acetaminophen overdose.
43
What is **Mercapturic acid**?
7. Mercapturic acid ## Footnote This is a product of the conjugation of glutathione with electrophilic compounds.
44
What is a **proton pump inhibitor**?
8. Proton pump inhibitor ## Footnote These drugs reduce gastric acid production by inhibiting the proton pump in the stomach lining.
45
What is **Piroxicam**?
9. Piroxicam ## Footnote Piroxicam is a nonsteroidal anti-inflammatory drug (NSAID) used to relieve pain and inflammation.
46
What is **Misoprostol**?
10. Misoprostol ## Footnote Misoprostol is a medication used to prevent gastric ulcers and induce labor.
47
What is a **Tertiary amine**?
11. Tertiary amine ## Footnote Tertiary amines are organic compounds with three alkyl or aryl groups attached to a nitrogen atom.
48
What is **Lipid soluble**?
12. Lipid soluble ## Footnote Lipid-soluble substances can easily pass through cell membranes and are often stored in fatty tissues.
49
What does it mean to **Cross BBB**?
13. Crosses BBB ## Footnote This refers to the ability of substances to penetrate the blood-brain barrier.
50
What is associated with **GI bleeding**?
14. GI bleeding ## Footnote This can be a side effect of certain medications, especially NSAIDs.
51
What are **Renal diseases**?
15. Renal diseases ## Footnote These are conditions that affect kidney function and can impact drug metabolism.
52
What is a **5HT3 antagonist**?
16. 5HT3 antagonist ## Footnote These drugs block serotonin receptors and are often used to prevent nausea and vomiting.
53
What is a **5HT 1B/1D agonist**?
17. 5HT 1B/1D agonist ## Footnote These are medications used to treat migraines by constricting blood vessels in the brain.
54
What is a **peptide opioid neurotransmitter**?
18. Peptide opioid neurotransmitter ## Footnote These include endorphins and enkephalins, which modulate pain and reward.
55
What is **Diacetyl morphine**?
19. Diacetyl morphine ## Footnote This is another name for heroin, an opioid drug.
56
What is **cysteine**?
20. Cysteine ## Footnote Cysteine is a sulfur-containing amino acid important for protein synthesis.
57
What is **glycine**?
21. Glycine ## Footnote Glycine is the simplest amino acid and acts as an inhibitory neurotransmitter.
58
What is **glutamic acid**?
22. Glutamic acid ## Footnote Glutamic acid is an amino acid that serves as a neurotransmitter in the brain.
59
What does **pinpoint pupil** indicate?
23. Pinpoint pupil ## Footnote This can be a sign of opioid overdose or exposure to certain toxins.
60
What is **respiratory depression**?
24. Respiratory depression ## Footnote This is a condition where breathing becomes inadequate, often due to opioid use.
61
What is **constipation** in relation to opioids?
25. Constipation ## Footnote Opioids commonly cause constipation as a side effect due to their action on the gastrointestinal tract.
62
What is a **Type 1 PG analog**?
26. Type 1 PG analog ## Footnote These are prostaglandin analogs that mimic the effects of natural prostaglandins.
63
What are **steroid sparing agents**?
27. Steroid sparing agents ## Footnote These medications help reduce the need for corticosteroids in treatment.
64
What is an **analgesic**?
28. Analgesic ## Footnote Analgesics are drugs that relieve pain without causing loss of consciousness.
65
What is an **antidiarrheal**?
29. Antidiarrheal ## Footnote Antidiarrheals are medications used to treat diarrhea by slowing down gut movement.
66
What is an **antitussive**?
30. Antitussive ## Footnote Antitussives are drugs that suppress coughing.
67
Histamine precursor is?
Histidine ## Footnote Histidine is converted to histamine by histidine decarboxylase.
68
Serotonin precursor of?
Tryptophan ## Footnote Tryptophan is an essential amino acid that is a precursor to serotonin.
69
1st generation antihistamines often cause sedation, this is due to?
Anticholinergic effects ## Footnote These effects can lead to drowsiness and sedation.
70
Ondansetron is classified as?
5HT3 antagonist ## Footnote Ondansetron is used to prevent nausea and vomiting.
71
Triptans is classified as?
5HT 1B/1D agonist ## Footnote Triptans are used to treat acute migraine attacks.
72
Latanoprost is classified as?
Prostaglandin analog ## Footnote Latanoprost is used to lower intraocular pressure in glaucoma.
73
Montelukast mechanism of action?
Leukotriene receptor antagonist ## Footnote Montelukast blocks the action of leukotrienes in the body.
74
Endorphins are?
Peptide opioid neurotransmitters ## Footnote Endorphins help to relieve pain and induce feelings of pleasure.
75
Ecosonide are?
Arachidonic acid derivatives ## Footnote Ecosonide is involved in inflammatory responses.
76
Misoprostol is?
Prostaglandin E1 analog ## Footnote Misoprostol is used for preventing gastric ulcers and inducing labor.
77
Acetaminophen hepatotoxicity is due to?
N-acetyl-p-benzoquinoneimine ## Footnote This toxic metabolite can cause liver damage.
78
Glutathione conjugation produce?
Mercapturic acid ## Footnote This process detoxifies harmful substances in the body.
79
The most common side effects associated with NSAIDs?
GI bleeding ## Footnote NSAIDs can irritate the gastrointestinal tract.
80
What NSAID has highest GI bleeding?
Piroxicam ## Footnote Piroxicam is known for its higher risk of gastrointestinal bleeding.
81
Drug of choice to treat NSAID induced GI ulcer?
Proton pump inhibitor ## Footnote Proton pump inhibitors are effective in healing NSAID-induced ulcers.
82
Drug of choice to prevent NSAID induced GI ulcer?
Misoprostol ## Footnote Misoprostol is used to prevent ulcers caused by NSAIDs.
83
Glutathione consists of?
Cysteine, glycine, glutamic acid ## Footnote Glutathione is a tripeptide that plays a crucial role in detoxification.
84
Ibuprofen, indomethacin, mefenamic acid are?
NSAIDs ## Footnote These drugs are used to relieve pain and inflammation.
85
Leukotriene antagonist also referred as?
Leukotriene receptor antagonist ## Footnote These drugs block the action of leukotrienes.
86
Opioids can be used as?
Analgesics ## Footnote Opioids are effective for managing severe pain.
87
Heroin structure?
Diacetyl morphine ## Footnote Heroin is chemically known as diacetyl morphine.
88
Morphine overdose symptoms?
Pinpoint pupils, respiratory depression, constipation ## Footnote These symptoms indicate severe opioid toxicity.
89
Glutathione is a tripeptide that contains unusual tripeptide linkage between?
Amino acids ## Footnote Glutathione consists of cysteine, glutamic acid, and glycine.
Serotonin histamine cology
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