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Musculoskeletal Exam 1 > Pharmacology - Prostaglandins and Autacoids > Flashcards

Pharmacology - Prostaglandins and Autacoids Flashcards

1
Q

What is an autacoid?

A

An endogenous compound secreted by one type of cell but its effect is to modulate function of another cell within the same area.

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2
Q

What are Eicosanoid’s function?

A
  • Function in the body, are also potential disease mediators.
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3
Q

What are the seven types of Eicosanoids?

A 
Prostaglandins( in endothelial cells)
Prostacycylins 
Thromboxane (Produced in platelets)
Leukotrienes (asthma)
Lipoxins
Isoprostanes
EETs
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4
Q

How are Eicosanoids created?

A

An inflammatory response–> Arachidonic acid is cleaved by phosolipase A and depending on the enzymes that its available in or the tissues its located in it will differentiate into a specific Eicosanoid

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5
Q

In arthritis (rheumatoid, osteoarthritis) what are the two main autacoids?

A

COX2 and PGE2

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6
Q

In asthma what are the 4 autacoids that are significant?

A

PGD2 and LTB4

LTC4 and LTD4

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7
Q

In Crohn’s disease and UC what are the main autacoids?

A
  • and increase in LTB4 in affected mucosa leading to leukocytes infiltration
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8
Q

In cancer what is the significance of autacoids?

A

only circumstancial evidence only

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9
Q

In Dysmenorrha what are the main autacoids?

A

Endometrium –> PGE2 and PGF2a

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10
Q

In Glomerulonephritis what are the main autacoids?

A

Abnormal elevation of LTB4 due to complement proteins. In cysteinyl leukotrienes there is a decrease in glomerular filtration.

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11
Q

In cardiovascular disease what are the autacoids that can make the condition worsen?

A
  • increased levels of thromboxane which will constrict blood vessels.
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12
Q

What Eicosanoids can Erectile dysfunction be treated with?

A
  • PGE1
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13
Q

What Eicosanoids are used for labor and abortion?

A

Induction of labor –>PGE2 and PGF2a

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14
Q

What Eicosanoid are used to treat Glaucoma?

A

PGE2 used to dilate increasing passage and allow vitreous humor to escape.

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15
Q

What Eicosanoid is used to keep a ductus arteriosus open?

A
  • PGE2
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16
Q

What Eicosanoid is used to treat pulmonary hypertension?

A

PGI2

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17
Q

What are the class of anti-Eicosanoids?

A

Corticosteroids (Prednisone, Dexamethasone)
NSAIDS (aspirin, indomethacin, ibuprofen)
Inhibitors of leukotrienes ( Zafirlukast, montelukast)
Inhibitors of thromboxanes (Dazoxiben, pirmagrel)

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18
Q

What is the mechanism of action of corticosteroids?

A

Decrease immune response and decrease inflammatory response - via an increased expression of IL-10 and receptors in the bronchials. They also increase the expression of IL-1 receptor antagonist thats main goal is to decrease expression of IL-2 - IL-6 (IL-4 stimulates beta cells to produce IgE with IL-5 are the potent recruiter of eosinophils (inflammation). Also inhibit cyclooxygenase inhibitors. Without phospholipase A will not have arachondonic acid inhibits phospholipase A indirectly via lipocortin.

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19
Q

What are some types of Corticosteroids?

A

Prednisone, betamethasone, dexamethasone, triamcinolone.

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20
Q

What are some clinical applications of Corticosteroids?

A

Asthma (inhaled formulations) - inhibition of IL-4 and IL-5. Will not treat just suppress

  • Arthritis (rheumatoid, osteoarthritis)
  • Systemic lupus erythematosus
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21
Q

What are some types of Thromboxane
antagonists?
- What are the clinical application?
What might an adverse effect be?

A

Dazoxiben, Pirmagrel, Ridogrel

  • Similar to aspirin
  • Bleeding
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22
Q

What are some common properties of NSAIDS?

What is the MOA?

A
  • Properties: Found in synovial fluid, inhibit platelets and suppress inflammation, analgesic and antipyretic, gastric irritation, nephrotoxity, and heptotoxicity (diclofenac and sulindac)
  • Nonselective COX inhibitor
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23
Q

What is the COX selectivity for NSAID?

A
  • COX1 > COX2 (indometacin, sulindac)
  • COX1 = COX2 (meclofenamate, ibuprofen)
  • COX1 < COX2 (celecoxib, rofecoxib)
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24
Q

What is the nmonemic for cox selectivity?

A

If you like 1 cox over 2 you are either in love or sullen. If you can’t decide if you want 1 cox or 2 you propably have a headache or meclofenamate, and if you like 2 cox rather than one you were probably celebrant and want it rofe!!

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25
Q

What are the clinical application for aspirin?

What is the MOA?

A
  • Mild to moderat pain, headache, myalgia, arthralgia, prophylaxis for stroke and myocardial infarction
  • Cox1 and Cox2 inhibition
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26
Q

What are the adversed effects of aspirin?

A
  • GI ULCERS
  • BLEEDING
  • asthma exacerbation
  • bronchospasm
  • angioedema
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27
Q

What are the types of propionic acid drugs?

What are the clinical applications to drugs that have propionic acid?

A
  • Ibuprofen, naproxen, ketoprofen, fluprofen

- mild to moderate pain, fever, Osteoarthritis, rheumatoid arthritis, dysmenorrhea, and gout

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28
Q

What are the adverse effects of drugs that use Propionic acid?

A
  • GI hemorrhage, ulceration, perforation, nephrotoxicity, stevens-johnsons syndrome ( immune reaction)
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29
Q

What are the Acetic acid derivatives of the anti-eicosanoids?

  • What are the clinical applications of drugs that are acetic acid derivatives?
  • What are the adverse effects?
A
  • Indomethacin, Sulindac, etodolac, diclofenac, ketorolac
  • Clinical app: long term treatment of rheumatoid arthritis, closure of patent ductus arterioles,
  • Adverse effects: GI disturbances, tinnitus
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30
Q

What types of drugs are oxicams?
What are they used for?
What are the adverse effects?

A
  • Piroxicam (bad b/c it can cause more GI bleeding than aspirin)
  • For Rheumatoid, osteoarthritis, primary dysmenorrhea
  • Adverse effects: GI bleeding > aspirin
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31
Q

What type of drug is a ketone anti-eicosanoid?

A
  • Nabumetone
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32
Q

What are some COX2 selective antagonist?

What are some clinical applications?

A

Celecoxib (only one used), Rofecoxib

-Osteoarthritis, rheumatoid arthritis, primary dysmenrrheal, acute pain in adults familial adenomatous polyposis.

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33
Q

What are some adverse effect of COX2 selective antagonist?

A
  • MYOCARDIAL INFARCTION
  • GI bleeding
  • peripheral edema
  • asthma
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34
Q

What are the applications and MOA of Acetaminophen?

What are some adverse effects?

A
  • Application: Fever mild to moderate pain
  • MOA: COX3 inhibition
  • Adverse effects: hepatotoxicity, nephrotoxicity and hypothermia
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35
Q

What is the only Lipoxygenase inhibitor that we need to freaking know and what the hell is it used for?
How can is Screw up your shit?

A
  • Zileuton: used for Asthma (not as effective as other forms of treatment)
  • Adverse effects: Urticaria (rash of round, red welts on skin that itch intensely), abdominal discomfort, dizziness, and insomnia.
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36
Q

What does lipoxygenase inhibitors do?

A
  • neutrophils produce lipoxygenase which converts arachdonic acid lipoxine
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37
Q

What are some LT receptor antagonists?

What are some clinical applications of LT (Leukotriene) receptor antagonists?

A
  • Montelukast and Zafirlukast

- Chronic asthma, perennial allergic rhinitis and seasonal allergic rhinitis (montelukast)

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38
Q

What are some adverse effects of LT receptor antagonists?

A
  • GI distress, hallucination and agitation, allergic granulomatosis angiitis, hepatitis
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39
Q

What are the two receptor types that can terminate pregnancy at any stage secondary to uterine contraction?

  • What is the one PGE2 drug used in the USA?
  • What does it do?
A
  • PGE2 and PGF2a
  • Dinoprostone
  • Obstetric: induction of labor at term (ripens the cervix), 2nd trimester abortion, missed abortion, benign hydatidiform mole.
  • Caution: prolonged vaginal bleeding and severe menstrual cramps occur if used for menstral regulation or early abortion
How well did you know this?
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40
Q

What type of drug is misoprostol?

  • What does it treat?
  • What does it need to be combined with to be an abortifacient?
A

“Morning after pill”

  • PGE1
  • Peptic ulcer
  • Mifepristone
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41
Q

What type of drug is carboprost?
What are it’s applications?
What are its adverse effect?

A
  • PGF2a agonists
  • 2nd trimester abortion, resistant postpartum hemorrhage
  • Adverse effects: GI distrubances, dystonia and Pulmonary edema
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42
Q

What can cause dysmenorrhea and what is its treatment?

A
  • High levels of PGE2 and PGF2a during menstruation leading to contraction of uterus resulting in menstrual pain. Dysmenorrhea is easily treated with NSAIDs
How well did you know this?
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43
Q

What does Alprostadil treat?

What is a possible adverse effect?

A
  • Alprostadil (PGE1) is a second line drug used to treat erectile dysfunction (ED). Administer via intravacernosal injection or urethral suppository.
  • May cause penile pain
How well did you know this?
1
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2
3
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5
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44
Q

What drugs can be used to treat pulmonary hypertension?

A
  • Treprostinil (PGI2) approved for treatment of pulmonary hypertension and administered by subcutaneous infusion
  • Epoprostenol (PGI2) - for pulmonary hypertension.(adverse effect- hypotension, rash, GI disturbances, muscle pain)
How well did you know this?
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45
Q

What is another name for PGI2?

What do PRE1 and PGI2 do?

A
  • Prostacycline

- Vasodilate ( PGE1 [penis] PGI2 [pulmonary|)

46
Q

What drug would you give to maintain the patent ductus arteriosus?

  • What are adverse effects of said drug?
  • When is said drug contraindicated?
A
  • Alprostadil (PGE1)
  • Side effects may include apnea, bradycardia, hypotension, and hyperpyrexia.
  • Contraindicated in sickle cell anemia
47
Q

What are the two Eicosanoid drugs effective against asthma?

A

Zafirlukast and montelukast are effective against asthma. Zileuton is not as effective even though it has been used.

48
Q

What are two groups of drugs used to treat Glaucoma/Ocular hypertension?

A
  • Latanoprost (stable long-acting PGF2a)

- Bimatoprost, travoprost, and unoprostone (newer focuses on decreasing pressure)

49
Q

What are some adverse effects of Ecinosoids that treat Glaucoma/ ocular hypertension?

A
  • IRREVERSIBLE BROWN PIGMENTATION of the iris and eyelashes, conjunctivitis, blurred vision, and drying eyes.
50
Q

Where is histamine synthesizes and stored?

A
  • Mast cells, basophils, neurons, cells of gastric mucosa, and cells in regenerative or rapidly growing tissues
51
Q

By what mechanisms is Histamine released?

A
  • Immunologic release: IgE/Fc-mediated –> type I allergic reaction
  • Mechanical: Na+ causes release of histamine from granules when mast cells are injured
  • Drug induced release (tubercurine, morphine, vancomycin [red man syndrome]) Venom
52
Q

What are the functions of endogenous histamine in the immune system?

A

Allergy and inflammation

53
Q

What is the function of endogenous histamine in the CNS?

A 
- Circadian rhythms, 
increase in wakefulness and decrease in appetite
-Thirst, ADH release & body temp
-Pain perception and bp control
Anxiety, aggression, & locomotion
54
Q

What does reaction does histamine have on the nervous system?
What reaction does Histamine have on the cardiovascular system?
What reaction does Histamine have on the Bronchiolar system?

A
  • Nervous system: Pain and itching (urticaria, bites and stings), H3 agonists decrease release Ach, amines and peptide transmitter in CNS and PNS.
  • Cardiovasc: decrease systolic and diastolic bp, increase heart rate and contractility, Vasodilation in endothelium, and Edema.
  • Bronch: constriction–> asthma
  • GI: Gastric acid secretion
55
Q

What effect does histamine have during anaphylaxis/ pregnancy?

A

histamine induced contractions

56
Q

What drugs are first generation antihistamine?

What are there big adverse effects?

A
  • Ethanolamines, Phenothiazine, piperazines, piperdines, alkylamines, ethelenediamine,
  • Sedation dizziness
57
Q

What are the secondary drugs?

A
  • Piperazine (Certirizine)
  • Alkylamines (Acrivastine)
  • Piperdine (Loratadine and Fexofenadine)-
  • PHTHLAZINONES (Axelastine)
58
Q

What are the uses and the advese effect of Certirizine?

A
  • Uses: Allergic rhitinitis, allergic urticaria

- Adverse effects (somnolence, dry mouth, headache, fatigue)

59
Q

What are the uses of Loratadine and Fexofenadine?

A

Allergic rhitinitis and urticaria

60
Q

What are the clinical uses of Azelastine?

A
  • Allergic conjunctivitis and rhitinitis
61
Q

What are 4 H2 blockers?

A

Cimetidine, Ranintidine, fomotidine, nisatidine

62
Q

What is a type of serotonin receptor agonist and what are its effects?
-What are its major advantage over benzodiazepines?

A
  • Buspirone: an anxiolytic agent that relieves anxiety without causing sedative, hypnotic, and euphoric effects.
  • Does not affect driving skills and causes less psychomotor impairment
63
Q

What are the side effects of serotonin agonist?

A
  • Tachycardia, palpitation, nervousness, GI distress, and paresthesia.
64
Q

The Serotonin receptor agonist triptans is used to treat what?
What can be its adverse effects?
When are they contraindicated?

A
  • Used to treat acute migraine and cluster headache attacks
  • May cause coronary artery vasospasm and are contraindicated in patients with coronary artery disease.
  • Contraindicated in hepatic and renal insufficiency
65
Q

What is the serotonin receptor agonist Tegaserod?

A

Tegaserod: effective treatment of irritable bowel syndrome

66
Q

What is the serotonin receptor antagonist Ondansetron useful in treating?

A

-useful in preventing nausea and vomiting with surgery and chemotherapy

67
Q

What are some common properties of NSAIDS?

What is the MOA?

A
  • Properties: Found in synovial fluid, inhibit platelets and suppress inflammation, analgesic and antipyretic, gastric irritation, nephrotoxity, and heptotoxicity (diclofenac and sulindac)
  • Nonselective COX inhibitor
68
Q

What is the COX selectivity for NSAID?

A
  • COX1 > COX2 (indometacin, sulindac)
  • COX1 = COX2 (meclofenamate, ibuprofen)
  • COX1 < COX2 (celecoxib, rofecoxib)
69
Q

What is the nmonemic for cox selectivity?

A

If you like 1 cox over 2 you are either in love (cause idomethacin fills the hole in your heart) or sullen. If you can’t decide if you want 1 cox or 2 you propably have a headache (ibuprofen) or a feminist (meclofenamate), and if you like 2 cox rather than one you were probably celebrant due to heartbreak (celecoxib adverse reaction is MI) or like it rough (rofecoxib)!!

70
Q

What are the clinical application for aspirin?

What is the MOA?

A
  • Mild to moderat pain, headache, myalgia, arthralgia, prophylaxis for stroke and myocardial infarction
  • Cox1 and Cox2 inhibition
71
Q

What are the adversed effects of aspirin?

A
  • GI ULCERS
  • BLEEDING
  • asthma exacerbation
  • bronchospasm
  • angioedema
72
Q

What are the types of propionic acid drugs?

What are the clinical applications to drugs that have propionic acid?

A
  • Ibuprofen, naproxen, ketoprofen, fluprofen

- mild to moderate pain, fever, Osteoarthritis, rheumatoid arthritis, dysmenorrhea, and gout

73
Q

What are the adverse effects of drugs that use Propionic acid?

A
  • GI hemorrhage, ulceration, perforation, nephrotoxicity, stevens-johnsons syndrome ( immune reaction)
74
Q

What are the Acetic acid derivatives of the anti-eicosanoids?

  • What are the clinical applications of drugs that are acetic acid derivatives?
  • What are the adverse effects?
A
  • Indomethacin, Sulindac, etodolac, diclofenac, ketorolac
  • Clinical app: long term treatment of rheumatoid arthritis, closure of patent ductus arterioles,
  • Adverse effects: GI disturbances, tinnitus
75
Q

What types of drugs are oxicams?
What are they used for?
What are the adverse effects?

A
  • Piroxicam (bad b/c it can cause more GI bleeding than aspirin)
  • For Rheumatoid, osteoarthritis, primary dysmenorrhea
  • Adverse effects: GI bleeding > aspirin
76
Q

What type of drug is a ketone anti-eicosanoid?

A
  • Nabumetone
77
Q

What are some COX2 selective antagonist?

What are some clinical applications?

A

Celecoxib (only one used), Rofecoxib

-Osteoarthritis, rheumatoid arthritis, primary dysmenrrheal, acute pain in adults familial adenomatous polyposis.

78
Q

What are some adverse effect of COX2 selective antagonist?

A
  • MYOCARDIAL INFARCTION
  • GI bleeding
  • peripheral edema
  • asthma
79
Q

What are the applications and MOA of Acetaminophen?

What are some adverse effects?

A
  • Application: Fever mild to moderate pain
  • MOA: COX3 inhibition
  • Adverse effects: hepatotoxicity, nephrotoxicity and hypothermia
80
Q

What is the only Lipoxygenase inhibitor that we need to freaking know and what the hell is it used for?
How can is Screw up your shit?

A
  • Zileuton: used for Asthma (not as effective as other forms of treatment)
  • Adverse effects: Urticaria (rash of round, red welts on skin that itch intensely), abdominal discomfort, dizziness, and insomnia.
81
Q

What does lipoxygenase inhibitors do?

A
  • neutrophils produce lipoxygenase which converts arachdonic acid lipoxine
82
Q

What are some LT receptor antagonists?

What are some clinical applications of LT (Leukotriene) receptor antagonists?

A
  • Montelukast and Zafirlukast

- Chronic asthma, perennial allergic rhinitis and seasonal allergic rhinitis (montelukast)

83
Q

What are some adverse effects of LT receptor antagonists?

A
  • GI distress, hallucination and agitation, allergic granulomatosis angiitis, hepatitis
84
Q

What are the two receptor types that can terminate pregnancy at any stage secondary to uterine contraction?

  • What is the one PGE2 drug used in the USA?
  • What does it do?
A
  • PGE2 and PGF2a
  • Dinoprostone
  • Obstetric: induction of labor at term (ripens the cervix), 2nd trimester abortion, missed abortion, benign hydatidiform mole.
  • Caution: prolonged vaginal bleeding and severe menstrual cramps occur if used for menstral regulation or early abortion
85
Q

What type of drug is misoprostol?

  • What does it treat?
  • What does it need to be combined with to be an abortifacient?
A

“Morning after pill”

  • PGE1
  • Peptic ulcer
  • Mifepristone
86
Q

What type of drug is carboprost?
What are it’s applications?
What are its adverse effect?

A
  • PGF2a agonists
  • 2nd trimester abortion, resistant postpartum hemorrhage
  • Adverse effects: GI distrubances, dystonia and Pulmonary edema
87
Q

What can cause dysmenorrhea and what is its treatment?

A
  • High levels of PGE2 and PGF2a during menstruation leading to contraction of uterus resulting in menstrual pain. Dysmenorrhea is easily treated with NSAIDs
88
Q

What does Alprostadil treat?

What is a possible adverse effect?

A
  • Alprostadil (PGE1) is a second line drug used to treat erectile dysfunction (ED). Administer via intravacernosal injection or urethral suppository.
  • May cause penile pain
89
Q

What drugs can be used to treat pulmonary hypertension?

A
  • Treprostinil (PGI2) approved for treatment of pulmonary hypertension and administered by subcutaneous infusion
  • Epoprostenol (PGI2) - for pulmonary hypertension.(adverse effect- hypotension, rash, GI disturbances, muscle pain)
90
Q

What is another name for PGI2?

What do PRE1 and PGI2 do?

A
  • Prostacycline

- Vasodilate ( PGE1 [penis] PGI2 [pulmonary|)

91
Q

What drug would you give to maintain the patent ductus arteriosus?

  • What are adverse effects of said drug?
  • When is said drug contraindicated?
A
  • Alprostadil (PGE1)
  • Side effects may include apnea, bradycardia, hypotension, and hyperpyrexia.
  • Contraindicated in sickle cell anemia
92
Q

What are the two Eicosanoid drugs effective against asthma?

A

Zafirlukast and montelukast are effective against asthma. Zileuton is not as effective even though it has been used.

93
Q

What are two groups of drugs used to treat Glaucoma/Ocular hypertension?

A
  • Latanoprost (stable long-acting PGF2a)

- Bimatoprost, travoprost, and unoprostone (newer focuses on decreasing pressure)

94
Q

What are some adverse effects of Ecinosoids that treat Glaucoma/ ocular hypertension?

A
  • IRREVERSIBLE BROWN PIGMENTATION of the iris and eyelashes, conjunctivitis, blurred vision, and drying eyes.
95
Q

Where is histamine synthesizes and stored?

A
  • Mast cells, basophils, neurons, cells of gastric mucosa, and cells in regenerative or rapidly growing tissues
96
Q

By what mechanisms is Histamine released?

A
  • Immunologic release: IgE/Fc-mediated –> type I allergic reaction
  • Mechanical: Na+ causes release of histamine from granules when mast cells are injured
  • Drug induced release (tubercurine, morphine, vancomycin [red man syndrome]) Venom
97
Q

What are the functions of endogenous histamine in the immune system?

A

Allergy and inflammation

98
Q

What is the function of endogenous histamine in the CNS?

A 
- Circadian rhythms, 
increase in wakefulness and decrease in appetite
-Thirst, ADH release & body temp
-Pain perception and bp control
Anxiety, aggression, & locomotion
99
Q

What does reaction does histamine have on the nervous system?
What reaction does Histamine have on the cardiovascular system?
What reaction does Histamine have on the Bronchiolar system?

A
  • Nervous system: Pain and itching (urticaria, bites and stings), H3 agonists decrease release Ach, amines and peptide transmitter in CNS and PNS.
  • Cardiovasc: decrease systolic and diastolic bp, increase heart rate and contractility, Vasodilation in endothelium, and Edema.
  • Bronch: constriction–> asthma
  • GI: Gastric acid secretion
100
Q

What effect does histamine have during anaphylaxis/ pregnancy?

A

histamine induced contractions

101
Q

What drugs are first generation antihistamine?

What are there big adverse effects?

A
  • Ethanolamines, Phenothiazine, piperazines, piperdines, alkylamines, ethelenediamine,
  • Sedation dizziness
102
Q

What are the secondary drugs?

A
  • Piperazine (Certirizine)
  • Alkylamines (Acrivastine)
  • Piperdine (Loratadine and Fexofenadine)-
  • PHTHLAZINONES (Axelastine)
103
Q

What are the uses and the advese effect of Certirizine?

A
  • Uses: Allergic rhitinitis, allergic urticaria

- Adverse effects (somnolence, dry mouth, headache, fatigue)

104
Q

What are the uses of Loratadine and Fexofenadine?

A

Allergic rhitinitis and urticaria

105
Q

What are the clinical uses of Azelastine?

A
  • Allergic conjunctivitis and rhitinitis
106
Q

What are 4 H2 blockers?

A

Cimetidine, Ranintidine, fomotidine, nisatidine

107
Q

What is a type of serotonin receptor agonist and what are its effects?
-What are its major advantage over benzodiazepines?

A
  • Buspirone: an anxiolytic agent that relieves anxiety without causing sedative, hypnotic, and euphoric effects.
  • Does not affect driving skills and causes less psychomotor impairment
108
Q

What are the side effects of serotonin agonist?

A
  • Tachycardia, palpitation, nervousness, GI distress, and paresthesia.
109
Q

The Serotonin receptor agonist triptans is used to treat what?
What can be its adverse effects?
When are they contraindicated?

A
  • Used to treat acute migraine and cluster headache attacks
  • May cause coronary artery vasospasm and are contraindicated in patients with coronary artery disease.
  • Contraindicated in hepatic and renal insufficiency
110
Q

What is the serotonin receptor agonist Tegaserod?

A

Tegaserod: effective treatment of irritable bowel syndrome

111
Q

What is the serotonin receptor antagonist Ondansetron useful in treating?

A

-useful in preventing nausea and vomiting with surgery and chemotherapy

Musculoskeletal Exam 1 (11 decks)

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