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Musculoskeletal System > Pharmacology I and II > Flashcards

Pharmacology I and II Flashcards

1
Q

What are autacoids?

A

They are released in the body for short term and they act through paracrine signaling
Definition: endogenous molecules secreted more than one type of cell and act on different types of cell
They act like local hormones, have short duration
-proinflammatory - so you want to inhibit the synthesis of autacoids for pharmacological action

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2
Q

Eicosanoids

A

They are related to each other because they come from arachidonic acids
They are potential disease mediators
Resulting products are dependent on tissue and enzymes present

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3
Q

Thromboxanes

A

Responsible for clotting (platelet aggregation and vasoconstriction)
released exclusively like platelets
synthesized by COX pathway
very harmful for cardiovascular disease

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4
Q

Leukotrienes

A

Allergic response
synthesized from AA from the Lipooxygenase pathway
involved in asthmatic reactions
sustain inflammatory response

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5
Q

Lipoxins and isoprostanes

A

are not involved in disease process

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6
Q

What are the eicosanoids?

A

prostaglandins (PE), prostacyclin, thromboxanes (TAX), leukotrienes (LTs), isoprostanes, liproxins

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7
Q

Cytokines

A

Interleukins and TNF

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8
Q

Protacyclins

A

exclusively released by endothelial cells of the vasculature

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9
Q

Phospholipase A2

A

Activated by inflammation
(TNF and gamma-IF)
cause the release of arachadonic acid from the cell membrane

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10
Q

AA gives rise to different eicosanoids

A

through different enzymes

housekeeping enzymes - Lipooxygenase, COX, cytp450 epoxygenases

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11
Q

COX pathway gives rise to which molecules

A

thromboxane, prostacylins, and prostaglandins

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12
Q

Interferon

A

Prevents the synthesis of prostacyclin and may produce ischemia (mediate vasoconstriction)

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13
Q

Arthritis (rheumatoid, osteoparthritis)

A

COX2 is induced
pathological signal
PGE2 - important in central rheumatoid arthritis

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14
Q

Prostaglandins

A

various effects

synthesized from AA in the COX pathway

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15
Q

PGE2

A

Vasodilator
Contraindication : lowers the threshold of pain - feel more pain
used as a vaginal supposition to dilate the cervix

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16
Q

Dysmenorrhea

A

mediated by PGE2

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17
Q

Erectile dysfunction

A

managed by PGE1 (ALPROSTADIL)
causes vasodilation
Inject 10 minutes before desired erection (can cause penile pain)

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18
Q

ALPROSTADIL

A

PGE1
TREAT ERECTILE DYSFUNCTION
causes vasodilation via intracavernosal injection
Second line drug for this

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19
Q

Glaucoma

A

PGE1 or 2
Effective in treating NARROW ANGLE GLAUCOMA
Causes increased opening of CANAL OF SCHELM

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20
Q

PGE1 or 2 treat narrow angle glucose

A

open canal of schelmm

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21
Q

Labor and abortion

A

Induction of labor by giving PGE2 and PGF2a

cause pain

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22
Q

DINOPROSTONE

A

PGE2
induce labor and abortion
cause cervical relaxation and uterine contraction

PGE2 can be used as a progesterone to induce labor

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23
Q

DINOPROST

A

PGF2a
also induces labor and abortion
cause uterine contraction

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24
Q

LTB4 (leukotriene)

A

mediate asthma, glumerelonephritis, and ulcerative colitis (leukocyte infiltration)

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25
Q

Cancer

A

Inhibitors of autacoids e.g. NSAIDs aspirin is associated with reducing the rates of colon cancer
but no direct association that autacoids induce cancer

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26
Q

Pulmonary hypertension

A

PGI2 is a vasodilator
inhibit platelet activation
Prostacyclin
These are administered by subcutaneous infusion

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27
Q

Glaucoma

A

condition that increases intraocular pressure
blocks the canal of schlemn
cannot drain aqueous humor that is constantly generated

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28
Q

Ductus arteriosus

A

open channel congenitally in the heart
in stances when opening is needed to be maintained, use prostaglandins to keep it open (use vasodilator) and closed (use vasoconstrictor)

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29
Q

PGI2 and prostacyclins

A

treat pulmonary hypertension
PGI2 via specific target effect - dilate vessels in lungs
TREPROSTINIL - administered by subcutaneous infusion
EPOPROSTENOL -> give hypotension, rash,Gi problems, and muscle pain
-synthetic PGI2

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30
Q

PGE1

A

glaucoma
erectile dysfunction
maintenance of patent ductus arteriosus -ALPROSTADIL - can cause apnea, bradycardia, hypotension

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31
Q

Angiotensins

A

target is angiotension II
use ACE inhibitors
treat hypertension

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32
Q

Neuropeptides

A

released with NE and adrenergic

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33
Q

Prostaglandins

A

Constrict/dilate blood vessels

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34
Q

Trigger inflammatory response

A

depends on location (what tissues) and

availability of certain enzymes

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35
Q

What are the housekeeping enzymes?

A

COX1

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36
Q

Asthma

A

PGD2 (patient feel more pain)

LTB4, C4, D4

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37
Q

Crohn’s disease

A

erosions of GI portions

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38
Q

Glumerulonephritis

A

Abnormal elevation of LTB4 complement proteins !!! complement deposition

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39
Q

Cysteinyl leukotrienes CysLT

A

decrease glomerular filtration

40
Q

Anti-eicosanoids

A

selective targeting is important

bonding

41
Q

Corticosteriods drugs

use classification by plasma half lives

A

PREDNISONE - short acting
DEXAMETHASONE and BETAMETHASONE- long acting
TRIAMCINOLONE-intermediate acting
classification may be via half life, mode of administration, ability to cross over barriers

42
Q

GLUCOCORTICOID agents

A

high anti-inflammatory potency- have a longer duration of action
inhalend

43
Q

Treat arthritis

A

Glucocorticoids

44
Q

Can’t use glucocorticoid for which disease?

A

Osteoarthritis

because prolonged use will cause osteoporosis

45
Q

Inhibitors of leukotrienes

A

Zafirlukast, motelukast,
Zileuton
Treat ASTHMA to inhibit the high inflammatory leukotrienes present

46
Q

Inhibitors of thromboxanes

A

Dazoxiben
Pirmagrel
Ridogrel
anti-clot formation like aspirin

Problem using this is the inability to clot but useful for ischemic disease prone patients
Contraindication: patients with hemophilia

ADVERSE EFFECT: BLEEDING

47
Q

Corticosteriod

A

large class of drugs
anti-inflammatory , anti-eicosanoid drugs
IMPORTANT IN TARGETING ARTHRITIS, ASTHMA, SYSTEMIC LUPUS ERYTHEMATOSUS
can be used in autoimmune diseases as a replacement therapy e.g. primary and secondary adrenal insufficiency (addision’s disease)

48
Q

MOA of corticosteriods

A

indirect inhibition of phospholipase A so no AA released for synthesis of thromboxanes and prostaglandins
Overall effect is to decrease immune and inflammatory response
Increase IL-10 expression (anti-inflammatory)
Increase expression of Beta 2 receptor in bronchioles (bronchodilation)
Increases expression of IL-1 receptor antagonist (inhibitoy) to control IL2-6
Decrease expression of IL2-4
IL-4 is important in mediating asthma through IgE effect from mast cells

49
Q

Triamcinolone

A

corticosteriod
can be aerosolized - mostly localizing in the respiratory (asthma)
swallowing -> 60% of the dose

50
Q

Corticosteriod will increase the expression of what protein that indirectly acts on PLPA

A

Lipocortin (annexin)

which inhibit PLPA

51
Q

NSAIDs drugs

A 
ASPIRIN
INDOMETHACIN -can close patent ductus arteriosus
IBUPROFEN
NEPROXEN
SULINDAC
COLECOXIB
52
Q

DAZOXIBEN/PIRAGREL/RIDOGREL

A

investigatory drugs of thromboxane inhibitors
DAZOXIBEN/PIRAGREL - inhibits TXA synthesis in platelets
RIDOGREL - inhibit TXA-a2

53
Q

NSAIDs action

A

used to treat all sorts of pain, inflammation, fever, arthritis
Aspirin is the only one out of the NSAIDs that is used for cardiovascular diseases, the other ones will most likely be for inflammation
COX selectivity is important

54
Q

Adverse effects of NSAIDs

A

gastric irritation
nephrotoxicity
hepatotoxicity (DICLOFENAC, SULINDAC)

55
Q

Non-selective COX inhibitors

A

ASPIRIN

56
Q

COX1 > COX2

A

INDOMETHACIN

SULINDAC

57
Q

COX1=COX2

A

MECLOFENAMATE

IBUPROFEN

58
Q

COX1<COX2

A 
COLECOXIB   (celebrex)
ROFECOXIB (vioxx)
KETONES (NABUMETONE) - treat arthritis
Less GI bleeding than most NSAIDs
Tx: arthritis- both forms, Useful in treating familial Adenomatous polyposis - which is a colon cancer with many polyps
Adverse  effects: INCREASES STROKE 
VIOXX causing MI
59
Q

ASPIRIN

A

COX1 and COX 2 inhibitors
COX2 inhibition leads to increased synthesis of aspirin-triggered lipoxins but negative inhibition feedback keeps this normal
Tx: mild-moderate pain, headache, myalgia, arthalgia (PAIN IN JOINTS), prophylaxis for stroke and MI (CARDIOVASCULAR)
(variety of conditions)
Adverse: GI ulcers, BLEEDING, asthma excervation, bronchospasm, angioedema

60
Q

Proprionic acid

A

IBUPROFEN
NAPROFEN
-PROFEN

COX1=COX2 INHIBITION
Tx: pain, fever, OSTEOARTHRITIS, RHEUMATOID, DYSMENORRHEA, GOUT
Adverse effect seen in STEVENS-JOHNSONS SYNDROME (cause skin to become itchy)- give acetaminophen

61
Q

STEVENS JOHNSON SYNDROME

A

skin itchy - adverse effect of ibuprofen

give acetaminophen

62
Q

ACETIC ACID

A 
INDOMETACIN 
SULIDAC 
COX1>COX2 inhibitor 
Tx: long term tx of RHEUMATOID ARTHRITIS, INDOMETHACIN close patent ductus arteriosus
Adverse effect: GI disturbances,
TINNITUS
63
Q

Oxicam

A

PIROXICAM
non-selective COX inhibitor
Tx: RHEUMATOID ARTHRITIS, OSTEOARTHRITIS, PRIMARY DYSMENORRHEA
Adverse: GI bleeding (more than aspirin) !!!!!!!!

64
Q

Acetaminophen

A 
COX3 inhibitor 
not true NSAIDs 
No effect on inflammation 
Tx. fever, pain NO INFLAMMATION
Adverse: hepatotoxicity, nephrotoxicity, hypothermia
65
Q

Acetaminophen and hepatotoxicity

A

•Enzyme polymorphism will affect how fast it will acetylate the byproduct of acetaminophen → needs to be glutathionated to be removed safely
◦ fast metabolizers or OD will become toxic

66
Q

Lipoxygenase inhibitors

A

Inhibition of lipotoxin, leukotrienes
ZILEUTON
Prevent neutrophil chemotaxis (infiltration of leukocytes) …The neutrophils which synthesize the enzymes in the pathway and produce release LT
Tx. ASTHMA via upstReam- not as effective drug as beta 2 AGONIST or receptor blockers
Adverse: HIVES - urticaria, insomnia, dizziness

NOT AS EFFECTIVE as MONTELUKAST, ZEFIRLUKAST due to specificity (AFFINITY?)
-> these are also leukotriene inhibitors but they are receptor blockers of LT

67
Q

LT RECEPTOR antagonist

A

MONTELUKAST
ZAFIRLUKAST
Treat ASTHMA downstream
Block CysLT1 receptors (reducing the constriction of airways, build-up of mucus, inflammation, or effect on glumerulus)
Tx: chronic asthma, seasonal allergic rhinitis
Adverse: GI distress, VASCULITIS (allergic granulomatous angitis), hallucination
GOOD EFFICACY

68
Q

Female Reproductive System Eicosanoids I

DINOPROSTONE

A

DINOPROSTONE - PGE2
Used for “ripening” the cervix and induce labor
CAN BE USED FOR 2ND TRIMESTER abortion
HYDATIDIFORM MOLE, and missed abortion
Advise: BLEEDING of the vagina, severe menstraul cramps

69
Q

Female Reproductive System Eicosanoids II MISOPROSTOL

A

Tx. NSAID induced peptic ulcer

****very effective abortificient agent when combined w/ mifepristone

70
Q

Morning after pill (MIFEPRISTONE)

A

MIFEPRISTONE - a progesterone receptor antagonist

71
Q

Female Reproductive System Eicosanoids II

CARBOPROST

A

PGF2a - potent vasocontrictor
2nd trimester abortion
Resist postpartum hemorrhage (vasoconstriction of the vessels)
Adverse: GI effects, Pulmonary edema

72
Q

Tx Dysmenorrhea

A

Using early NSAID
IBUPROFEN
Proponoic acid

73
Q

PDA

A

when treated with PGE1 ALPROSTADIL

-contradict with sickle cell anemia if tx patent ductus arteriosus

74
Q

PGI2

A

can cause paradoxical pulmonary hypertension while treating pulm hypertension

75
Q

PGF2 TREATING NARROW ANGLE GLAUCOMA

A

LATANOPROST, (new drugs: TRAVOPROST, UNPROSTONE)
LONG ACTING
used as DROPS
Can cause IRREVIERSIBLE PIGMENTATION OF THE EYES, conjunctivitis, drying eyes

Accelerates the exertion of aqueous humor

76
Q

Tx Crohn’s disease or ulcerative colitis

A

Autoimmune erosion of the GI tract
Corticosteriod can block production of leukotriene responsible for the leukocyte infiltration in the mucosa

  • stops the damaging inflammatory response
77
Q

Histamine - autacoids

A

Made significantly in mast cells and basophils, and enterochromaffin-like cells of gastric muscosa
in response to allergens - Act on smooth muscles

High amounts in the lungs
Preformed IgE/Fc-mediated release due to allergic response will cause type I response

78
Q

CNS effect of Histamine

A

Effects circadian rhythm
Increase wakefulness
Decrease appetite, thirst, ADH release, body temperature, pain perception
BP control , anxiety, aggression, locomotion

79
Q

Which drugs will increase the release of histamine?

A

Tubercurine
Morphine
Vancomycin - CAUSE REDMAN SYNDROME
venom

80
Q

What mechanical stimulus will increase release of histamine?

A

Na+ causes release of histamine from granules

-when cells are damaged

81
Q

Histamine functions

A

Allergy and inflammation -Anaphylaxis
Gastric acid secretion
Histamin-induced contractions in pregnancy

82
Q

Pathophysiology of Histamine

A

Nervous (H1, H2): pain and itching (hives, bites, stings)
H2 agonists decrease release of Ach, amines, and peptide transmitter
Cardiovascular (H2): decrease bp, increase HR and contractility
Bronchiolar (H1): constriction - asthma
GI Tract (H2): gastric acid secretion

83
Q

1st generation Anti-Histamines are inverse agonists

A

Tx. rhitnitis, condunctivitis, uritcaria (hives)
parkinsonism, motion sickness, INSOMNIA (cross BBB)
Adverse: sedation, dizziness, dry eyes, dry mouth, urinary retention,
Contraindications: narrow angle glaucoma, peptic ulcer

84
Q

1st generation Anti-histamins

A 
ETHANOLAMINES (-AMINE)
PHENOTHIAZINE
HYDROXYZINE, CYCLIZINE, MECLIZINE
CYPROHETADINE, PHENINDAMINE
ALKYLAMINES (CHLORO AND BROM-AMINE)
ETHELENEDIAMINE (PYRILAMINE, TRIPELEAMINE)
85
Q

2nd generation Anti-histamines

**just memorize these

A

Piperazine or CERTIRIZINE
Tx : allergic rhyinitis, allergic urticaria
Adverse: somnolence, dry bout, headache, fatigue
Alylamines - ACRIVASTINE
Tx: allergic rhynitis
Piperidine - LORATADINE, FEXOFENADINE
Tx: allergic rhyinitis, allergic urticaria

86
Q

H2 Blockers

A

CIMETIDINE - work on enterochromaffin-like cells in GI (not that effective)
RANINTIDEIN
FAMOTIDINE
NISATIDINE
Tx: stomach acid
Adverse: diarrhea, headache, fatigue, constipation

87
Q

REDMAN SYNDROME

A

vancomycin causes this due to release of high histamine

88
Q

1st generation of Anti- Histamine drugs cross what?

A

BBB due to non-ionization at blood pH
cause drowsiness
can cause anti-emetic due to affect on neurons

89
Q

Tx Allergy and insomnia with what generation of anti-histamine?

A

1st generation

90
Q

Cardiovascular effects of histamine

A

can be both contractor and dilator depending on which tissue bed it acts on

Increase HR, BP - H2
Vasodilation - H1 coupled to NO in the endothelium
Edema (hives)

91
Q

Serotonin 5HT receptor agonist

A

Less PSYCHOMOTOR effects than antihistamine drugs and benzodiapezines

92
Q

5HT receptor agonists I

BUSPIRONE 5HT1A

A

BUSPIRONE
PARTIAL AGONIST
NON BENZODIAPEPINE SELECTIVE
Relieves anxiety without euphoria, sedation
Does not affect driving skills
Adverse: tachycardia, palpitation, nervousness, paresthesia

93
Q

5HT receptor agonist II **TRIPTANS

SUMATRIPTAN 5HT1D/1B

A

Tx: acute migraine and cluster headache attacks
Contraindication: coronary artery vasospasm
hepatic and renal insufficiency (NARATRIPTAN, ELETRIPTAN)

94
Q

5HT receptor agonist III

CISAPRIDE AND TEGASEROD 5HT4

A

Tx. irritable bowel syndrome w/ constipation

Don’t use CISAPRIDE DISAPRIDE

95
Q

ONDANSTERONE

A

is a 5HT RECEPTOR ANTAGONIST

e.g. prevent nausea and vomitting W/ CHEMO

96
Q

Adverse effects of antihistamine (1st and 2nd generation comparison)

A

1st generation: sedation, dizziness,
2nd generation: headache, fatigue
both: dry eyes and mouth

Musculoskeletal System (27 decks)

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