Pharm Block 1

Front 1

What are the four 1st generation H1 Antagonists (antihistamines)?

Back 1

Dimenhydrinate

Diphenhydramine

Promethazine

Meclizine

Front 2

Promethazine is a 1st Generation H1 Antagonist (antihistamine) that blocks which other type of receptor?

Back 2

Promethazine can also block Alpha-1

Front 3

What are the three main actions of 1st Generation H1 Antagonists (antihistamines)?

Back 3

1. Allergy alleviation

2. Motion sickness alleviation (antiemetic)

3. Sedative/Sleep Aid

Front 4

What are the five toxicities associated with 1st generation H1 Antagonists?

Back 4

1. Sedation

2. Anti-muscarinic (treats motion sickness)

3. Alpha-1 antagonists

4. Blurred vision (contraindicated for glaucoma)

5. Urinary Retention (contraindictated for BPH)

Front 5

What are the five 2nd generation H1 Antagonists (antihistamines)?

Back 5

1. Loratadine

2. Desloratadine

3. Fexofenadine

4. Cetirizine

5. Levocetirizine

Front 6

2nd generation H1 Antagonists are mainly used to treat what?

Back 6

Allergies

Front 7

2nd generation H1 Antagonists are useless for what condition?

Back 7

Motion sickness since there is no antiemetic effect.

Front 8

Activation of what releases Serotonin? What effect does Serotonin have in most arterioles?

Back 8

Activation of platelets.

Vasoconstrictive effect in most arterioles.

Front 9

1. Serotonin can be metabolized to what? Where?

2. Elimination of Serotonin requires oxidation by what enzyme?

Back 9

1. Serotonin can be metabolized to Melatonin in the Pineal gland.

2. Elimination of Serotonin requires oxidation by monoamine oxidase (MAO).

Front 10

What is a Carcinoid Tumor? What does it release large amounts of?

Back 10

A neoplasm of ECLs that release great amounts of Serotonin.

Front 11

What are the initial symptoms of a Carcinoid Tumor?

Back 11

Uncomfortable flushing of the head/neck, abdominal cramps, and diarrhea.

Wheezing and erectile dysfunction may occur.

Front 12

1. How is diagnosis of a Carcinoid Tumor accomplished?

2. What kind of drug category can suppress the symptoms prior to surgical removal of the tumor?

Back 12

1. By measuring 5-hydroxyindoleacetic acid (5-HIAA), which is a Serotonin metabolite in the urine.

2. 5-HT2 antagonists can suppress the symptoms.

Front 13

1. What is Serotonin Syndrome?

2. What kind of 4 drugs could cause it?

Back 13

1. Excess of Serotonin in the body induced by drugs.

2. Seratonin metabolism blockers (MAOI), SSRIs, Tricyclic antidepressants, and Serotonin agonists.

Front 14

1. What are the symptoms of Serotonin Syndrome?

2. What are two treatments for it?

Back 14

1. Hypertension, Hyperflexia, Hyperthermia (resulting from skeletal muscle hyperactivity), diarrhea, coma, clonus (muscle spasms), mydriasis (pupil dilation).

2. You can use a 5-HT2 antagonist (e.g. Cyproheptadine). Another treatment is sedation and neuromuscular paralysis with respiratory intubation can be beneficial.

Front 15

5-HT2A is a Serotonin receptor. What is its MOA?

*Its MOA is a 2nd messenger mechanism.

Back 15

Gq --> IP3 --> Calcium increase

Front 16

Serotonin with its 5-HT2A are found in which two tissue sites?

Back 16

1. Platelet storage

2. Smooth muscle (not including heart, or blood vessels in skeletal muscle).

Front 17

What are the 3 actions of Serotonin via the 5-HT2A receptor in smooth muscle (not including blood vessels of skeletal muscle, or heart?)

Back 17

1. Bronchiolar tone

2. G.I. tone (contraction) --> Peristalsis

3. Vasoconstriction

Front 18

What is the main toxicity of Serotonin via the 5-HT2A receptor?

Back 18

Serotonin Syndrome

Front 19

1. What is the MOA of Serotonin via the 5-HT3 receptor?

2. What are the two sites of action for Serotonin via the 5-HT3 receptor?

Back 19

1. Na+/K+ channel activation

2. G.I tract, and CTZ (chemoreceptor trigger zone of medulla).

Front 20

What is the main action of Serotonin via the 5-HT3 receptor?

Back 20

Vomiting reflex caused by chemical stimuli (e.g. chemotherapy)

Front 21

1. What are the 3 drugs considered Serotonin Antagonists at the 5-HT2A receptor?

2. Which of the three serves solely as a platelet stabilizer?

Back 21

1. Cyproheptadine

2. Phenoxybenzamine

3. Ritanserin - platelet stabilizer

Front 22

1. What are the actions shared by Cyproheptadine and Phenoxybenzamine?

2. What are their shared 3 toxicities?

3. These two drugs can serve as blockers of what other type of receptor?

Back 22

1. Both are 5-HT2A antagonists which act on smooth muscle in carcinoid tumors.

2. Cold-induced urticarial (hives), sedative, anti-muscarinic.

3. H1 blockers

Front 23

In Asthma and COPD, the action of Serotonin is blocked by what category of drugs?

Back 23

Beta-2 agonists

Front 24

What is Bradykinin and its general function?

Back 24

Bradykinin is an inflammatory mediator. It is a peptide that causes blood vessels to dilate, and therefore causes blood pressure to fall.

Front 25

What are the actions and toxicities of B1 and B2 receptors of Bradykinin?

Back 25

1a. B1 = proinflammatory action

1b. B1 tox = pain, edema

2a. B2 = bronchoconstriction, vasodilation

2b. B2 tox = Asthma, COPD, inflammatory hyperemia, hypotension.

Front 26

Increased Bradykinin with ACE inhibitors, produces what two effects?

Back 26

Cough, angioedema

Front 27

Histamine H1 receptor has what kind of 2nd messenger MOA in both sensory nerves and bronchioles?

Back 27

Gq --> IP3 --> Calcium increase

Front 28

Histamine H1 receptor in arterioles/venules have what kind of MOA?

Back 28

Nitric Oxide

Front 29

What are the Histamine H1 receptor actions for:

1. Sensory nerves (2 actions)

2. Bronchioles (1 action)

3. Arterioles/Venules (3 actions)

Back 29

1. Pain, Itch

2. Bronchoconstriction

3. Dilation, leakage, edema

Front 30

What are the toxicities associated with the following tissue sites for Histamine H1 receptors:

1. Sensory nerves (2 tox)

2. Bronchioles (1 tox)

3. Arterioles/Venules (3 tox)

Back 30

1. Inflammatory response (redness, swelling), and Urticaria (hives)

2. Bronchospasm in asthma

3. Hypotension, tachycardia, headache

Front 31

Histamine H2 receptor is mainly found in the stomach. What is the MOA, Action, and 2 toxities?

Back 31

MOA = Gs --> cAMP increase

Action = Parietal Cell acid release

Tox = erosion, ulcers

Front 32

Beta-2 agonists are useful against Histamine actions. What are the two non-selective Beta-2 agonists that blocks all smooth muscle contraction (e.g. bronchoconstriction)?

Back 32

Epinephrine and Ephedrine

Front 33

Epinephrine and Ephedrine are non-selective Beta-2 agonists. What are their 2 main toxicities?

*Epinephrine has 2 additional CNS toxicities. What are they?

Back 33

1. Skeletal muscle tremors and cardiac palpitations.

2. Epinephrine can cause CNS excitement & hypertension.

Front 34

What are the names of the two selective Beta-2 agonists, their action, and 2 toxicities?

Back 34

1. Albuterol and Salmeterol

2. Antagonism of all smooth muscle contraction (e.g. bronchoconstriction).

3. Toxicities are skeletal muscle tremors, and cardiac palpitations.

*Tox is the same as non-selective Beta-2 agonists.

Front 35

What are the names of the two Beta-2 agonists that stabilize Mast Cells against IgE stimulation? Any toxicity?

Back 35

1. Cromolyn and Nedocromil.

2. No tox! Very safely inhaled and not absorbed.