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Pharmacology Test Two > Corticosteroids, AED, GI (+ very few Abx) > Flashcards

Corticosteroids, AED, GI (+ very few Abx) Flashcards

1
Q

What class of drug is caffeine

A

Methylxanthine

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2
Q

What kind of effect does caffeine have on dogs

A

Mild CNS stimulation, moderate bronchodilation

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3
Q

What class of drug is theophylline?

A

Methylxanthine

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4
Q

What effect does theophylline have

A

Bronchodilator

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5
Q

What is a side effect of methylxanthines (give examples)

A

CNS overstimulation (caffeine, theophylline)

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6
Q

What are cortocosteroids

A

Group of natural and synthetic substances mimicing the actions of cortisol

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7
Q

What actions are therapeutic used of cortocosteroids base on

A

Glucocorticoids (rather than mineralocorticoids)

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8
Q

What group of drugs causes anti-inflammation, imuunosuppression, metabolic changes, electrolyte balance and cardiovascular homeostasis?

A

cortocosteroids

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9
Q

Name the physio effects of cortocosteroids

A

anti-inflammation, imuunosuppression, metabolic changes, electrolyte balance and cardiovascular homeostasis

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10
Q

What are the effects of low, medium and high doses of cortocosteroids

A

Low - replacement Rx for adrenal insufficiency Medium- antiinflammatory High- immunosuppression

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11
Q

What is the most widely used class of drugs in veterinary medicine

A

cortocosteroids (and over used!)

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12
Q

What causes a delayed response in corticosteroids

A

Takes hours due to requirement of protein synthesis

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13
Q

What drug class will treat addisions disease

A

cortocosteroids

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14
Q

Describe the HPA

A

CNS stimulation signals they hypothalamus which releases CRH to the pituitary gland, which releases ACTH to adrenal gland, which produces cortisol. Cortisol has negative feedback onpititary and hypothalamus production of hormones

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15
Q

What can treat hyperactivation of the HPA axis

A

Trilostant (vetoryl) inhibits enzyme in the adrenal cortex to decrease cortisol synthesis

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16
Q

What are the paths of glucocorticoid actions

A
  1. genomic response to alter protein synthesis (slow- medium) 2/3 - non-genomic response to receptors in cytosol and on membrane
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17
Q

Describe the effects of glucocorticoids on carbohydrate metabolism

A

Increased glyconeogenesis and decreased cellular glucose use leading to hyperglycemia

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18
Q

Describe the effects of glucocorticoids on protein

A

Catabolism - amino acids sent to gluconeogenesis- protein loss from bone can cause osteoporosis, thnning of skin, delayed healing, muscle wasting

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19
Q

Describe the effects of glucocorticoids on fatty acid

A

Mobilizatioon from adipose

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20
Q

How do corticosteroids affect the inflammatory cascade

A

At high doses, decrease of enzyme activity, leukocyte infiltration and vasoactive/chemotactic factors leading to block of cascade

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21
Q

Describe the effects of glucocorticoids on electrolytes

A

Na retention, loss of K and Ca, decreased ADH leads to PUPD

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22
Q

Why should glucocorticoids be withdrawn slowly

A

HPAA suppression due to exogenous

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23
Q

What are the side effects of glucocorticoids (name 7)

A

Protein catabolism HPAA suppression Immunosuppression GI ulceration due to loss of GI protectant Diabetes Hypothryoidism Electrolyte imblance

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24
Q

Name the chemistry changes that are from glucocorticoids (4)

A

Glucosuria, increased cholesterol, decreased potassium, decreased thyroid

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25
Q

Do glucocorticoids treat cushings or addisons

A

Treat Addisons (hypo)- can push into iatrogenic Cushings (hyper)

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26
Q

What are the contraindications for glucocorticoids

A

Pre-existing bacterial/fungal/viral infections, pregnancy, diabetes (causes insulin resistance), renal disease/heart failure (due to fluid overload), young animals and GI ulcers

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27
Q

What are the four classes of glucocorticoids

A

A- short acting B- intermediate C- long acting D- not defined

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28
Q

What class of glucocorticoids does prednisone fall into?

A

A- short acting

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29
Q

What class of glucocorticoids does dexamethasone fall into?

A

C- long acting

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30
Q

What are the routes of glucocorticoid use

A

Topica, inhaled, oral, systemic

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31
Q

What is the elimination route of glucocorticoids

A

Hepatic

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32
Q

What effect does the moiety of corticosteroids have?

A

Side chains/esters delay metabolism and enhance duration of metabolism

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33
Q

Describe the pharmacodynamics of corticosteroids. What can affect this

A

PD does not match PKinetics - bio actions are longer lasting than their levels in plasma (different plasma and biologic half time). Different ester or free alcohol additions can change the biological half life

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34
Q

What determines the effect duration of corticosteroids

A

Ester form used

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35
Q

Describe effects of ester solubility on corticosteroids

A

highly soluble esters allow fast absorption (minutes to hours) moderately insoluble esters absorb over days to weeks poorly soluble esters absorb over weeks to months

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36
Q

What is the most widely used corticosteroid agent across species

A

Dexamethasone

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37
Q

What is the duration of dexamethason

A

Long acting

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38
Q

What is the main activity of dexamethasone

A

Glucocorticoid (little mineralo)

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39
Q

What is the benefit of corticosteroids that display primarily glucocorticoid actions

A

Less effect on fluid balance

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40
Q

What are the additional side effects of dexamethasone

A

Colonic perforation and laminitis in horses

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41
Q

What are the routes of administration of dexamethasone

A

PO, IM, IV, topical/ophtho

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42
Q

What is a synthetic drug which has more mineralocorticoid activity than other sythetic agents of the same type

A

Prednisone/solone

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43
Q

Describe the difference between pred/prednisolone

A

Prednisone is converted to prednisolone in the liver

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44
Q

Why would one Rx -P’solone over pred?

A

P’solone is easier on the liver (cats and horses especially)

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45
Q

Which animals are recommended to use P’‘solone over pred?

A

Horses and cats

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46
Q

Fat cats vs skinny cats- prednisone vs ‘solone

A

Fat cats ok to give prednosone

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47
Q

What corticosteroid can be given to a cat with liver and heart failure and why

A

methyl-prednisolone- devoid of mineralocorticoid activity and -solone easier on liver

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48
Q

What are the UFVH formulary warnings for prednisone

A

Do not use in animals with severe bacterial or fungal infections

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49
Q

What are the UFVH formulary warnings for dexamethasone

A

May cause laminitis in horses, GI bleeding or colonic perforation

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50
Q

What are the UFVH formulary warnings for prednisolone

A

Do not use in animals with corneal ulceration

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51
Q

What change in dose is necessary in corticosteroids in stressed animals

A

Dose may need to be increased as body would normally increase

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52
Q

What is the dose for prednisone anti-inflammatory

A

1 mg/kg/day

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53
Q

What is the dose for dexamethasone

A

1/7th prednisone - (1 mg/kg/day)/7

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54
Q

After what duration of time should corticosteroids be slowly withdrawn

A

After more than 1-2 weeks of use

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55
Q

What methods can be used to prevent gastric ulceration

A

Buffer stomach acid, inhibit receptors or inhibit H/K ATPase

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56
Q

What are the advantages and drawbacks of antacids

A

Inexpensive but frequent administration needed, can cause diarrhea (magnesium/maalox) or alkylosis (sodium bicarbonate)

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57
Q

Name a drug interaction for antacids

A

Enrofloxacin

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58
Q

What kind of Rx is famotidine

A

H2 inhibitor - prevent gastric ulceration

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59
Q

What kind of Rx is ranitidine

A

H2 inhibitor - prevent gastric ulceration, + prokinetic *think ran through the gut (zantac)

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60
Q

What kind of Rx is omeprazole

A

PPI- H/K ATPase (proton pump) inhibitors - prevent gastric ulceration

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61
Q

What common cautions are there with H2 inhibitors preventing gastric ulceration

A

Liver, +/- competition for p450 enzymes

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62
Q

How frequently should ranitidine be given

A

BID

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63
Q

How frequently should famotidine be given

A

BID

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64
Q

What side effects does ranitidine have?

A

Slight interference with p450 in the liver

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65
Q

What side effects does famotidine have

A

Liver complications but no interference with p450

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66
Q

*What replacement drug could be given in place of famotidine or ranitidine in liver failure patients

A

Nizatidine - no interference with p450

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67
Q

What kind of drugs are omeprazole, pantoprazole, lansoprazole

A

PPI (H/K ATPase) - to prevent gastric ulceration

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68
Q

What is the mechanism of PPI drugs

A

Reacts with active ATPase to inhibit H/K Pump

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69
Q

How should PPI drugs be given

A

Give 30 minute before meal, give in intact capsule or tablet with bicarbonate because they interact with gastric acid

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70
Q

What kind of drug is omeprazole

A

PPI- to prevent gastric ulceration

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71
Q

Which PPI can be given IV

A

pantoprazole

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72
Q

Which H2 inhibitor can be given IV

A

Famotidine

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73
Q

Which PPI is ok to split tablets?

A

Omeprazole

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74
Q

What is an advantage of Lansoprazole

A

Formulated with HCO3 as an oral liquid for dogs

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75
Q

What is an advantage of pantoprazole?

A

Can be given IV in anorexic patients

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76
Q

What kind of drug is mistoprostol

A

PGE1 (prostaglandin) analog - to prevent gastric ulceration

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77
Q

What drug is best in response to NSAID toxicity

A

Mistoprostol (wont help with hemorrhage from prednisone)

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78
Q

What are the effects of mistoprostol

A

Mimics prostaglandins Low dose- stimulates blood flow High dose- antacid

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79
Q

What is a side effect of mistoprostol

A

Can induce labor or abortion (PGE1 analog gastric ulcer preventative)

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80
Q

What kind of drug is sucralfate

A

Mucosal coating chelating and complexing agent to prevent gastric ulcer

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81
Q

Describe the mechanism of action of sucralfate

A

Prodrug which is converted by acid into a sugar polymer that coats stomach lesions and works as an antacid

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82
Q

What interactions are reported with sucralfate

A

Aluminum inhibits enrofloxacin so it should be given 1-2 hours before or more than 6 hours after sucralfate is given

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83
Q

*What are good sources of omega three fatty acids

A

Fish oil (EPA and DHA), linseed oil (a-linoleic acid)

84
Q

What kind of drugs are cisapride and mosapride

A

Prokinetics

85
Q

What is a precaution to note in cisapride

A

This prokinetic enhances reduced motility in stressed patients or those on steroids (due to slow gastric emptying)

86
Q

What is the function and mechanism of H2 inhibitors

A

H2 receptors are found on parietal cells which secrete acid

87
Q

What enzyme do prokinetics work on?

A

acetyl cholinesterase

88
Q

What precautions must be taken with PPIs

A

Gastrin build up can occur, so must wean off

89
Q

What are the two models for vomiting

A

Vomiting center in reticular formation CRTZ (chemoreceptor trigger zone) on floor of ventricle in dorsal medulla

90
Q

What types of drugs induce emesis

A

Dopamine agonist Adrenergic alpha agonists Gastric irritants

91
Q

What kind of drug is apomorphine

A

Dopamine agonist emesis inducer

92
Q

What is the mechanism of apomorphiine

A

Dopamine agonist which acts through the CRTZ

93
Q

Why might apomorphine not work in cats

A

They may not have dopamine receptors in CRTZ

94
Q

What type of drug is xylazine

A

Emesis inductor via alpha adrenergic agonism

95
Q

What type of drugs are ipecac and H2O2

A

Gastric irritant inducers of emesis

96
Q

What receptors are targeted in anti-emetics

A
  • Antimuscarinics (weak antiemetic) - Alpha 2 antagonists - NK1 receptor antagonists - Dopamine antagonists - 5HT3 antagonists
97
Q

What kind of drug is Centrine

A

antiemetic non-specific antimuscarinic

98
Q

What is the mechanism of Centrine

A

Antimuscarinic which reduces small intestinal motility and gastric emptying

99
Q

What is a drug interaction of Centrine

A

Blocks prokinetics

100
Q

What kind of drugs are chlorpromazine, prochlorperazine, acepromazine?

A

Antiemetics : Phenothiazines - alpha 2 antagonists

101
Q

What kind of drug is cerenia

A

Antiemetic- NK1 (neurokinin) receptor antagonist in vomiting center

102
Q

What is the drug name for cerenia

A

Maropitant

103
Q

What drug type is safe to combine with maropitant

A

5HT3 antagonists (maropitant is cerenia)

104
Q

What drug interactions are noted in maropitant

A

Ca channel blockers, cisapride (prokinetic), cyclosporine

105
Q

What type of drug is metoclopramide and what does it target

A

Antiemetic- dopamine agonist in CTZ Prokinetic- 5HT4 agonist

106
Q

What cautions should be noted in metoclopramide

A

Crosses BBB and can cause tremor

107
Q

*What Dopamine antagonist would be a good alternative to metoclopramide in neuro patients?

A

Domperidone - because it does not cross the BBB

108
Q

What is the effect and mechanism of 5HT3 antagonists

A

Anti-emetic - CTZ and vagal afferents from stomach

109
Q

What kind of drug is ondansetron

A

5HT3 anti-emetic

110
Q

What are the receptors involved in motion sickness anti-emetic drugs

A

-Inhibition of: + M1 (acetyl choline) in vestibular and CRTZ + H1 in vestibular apparatus

111
Q

What does inhibiting M1 and H1 receptors do

A

Control motion sickness

112
Q

What drugs should be used for chemotherapy associated emesis

A

Ondansetron and other 5HT3 antagonists

113
Q

*What is a less expensive option of 5HT3

A

Mirtazipine (instead of ondansetron)

114
Q

What effect does blocking cholinergics by centrine have?

A

Prokinetics

115
Q

What is the mechanism and effects of metaclopramide

A

Increases tone in esophageal sphincter, relaxes pylorus, and romotes gastric emptying (cholinergic 5HT4 agonist) Antiemetic (dopamine antagonists)

116
Q

What kind of drug is cisapride

A

mixed 5HT3 antagonist/5HT4 agonist, prokinetic

117
Q

What is the mechanism of action of cisapride

A

Prokinetic via release of acetyl choline to smooth muscle of intestine

118
Q

What are cautions in cisapride

A

Prolongs QT interval to cause fatal dysrhythmias in humans and boxers Obstipation in cats

119
Q

What drug should be used to reduce reflux during anesthesia in dogs?

A

Cisapride

120
Q

*What kind of drug is bethanacol

A

Muscarinic agonist prokinetic

121
Q

What is a side effect of bethanacol

A

Ineffective unless at high doses when SLUD occurs

122
Q

What are the two types of motility rhythms

A

*** and house keeper contractions

123
Q

What secondary effect does a 1/10th dose of erythromycin produce and why

A

Prokinetic via motilin agonist action on housekeeper contraction

124
Q

What secondary effect do ranitidine and nizatidine have

A

Prokinetic

125
Q

What drug should be used as a thoracic epidural analgesic for post operative ileus?

A

Lidocaine

126
Q

*What can be used to help with ileus in canines due to action on GI hormones?

A

Octreotide

127
Q

What effect do morphine agonist antidiarrheals have

A

Promotes segmental (mixing) contractions but not propagating (propulsive) - this slows transit and aids absorption

128
Q

What is the usual origin of diarrhea in dogs

A

Osmotic

129
Q

What kind of drugs are loperamide and diphenoxalate

A

Weak central action morphine agonist antidiarrheals loperamider (immodium) diphenoxalate (lomotil)

130
Q

What secondary effect does diphenoxalate

A

Diphenoxalate (lomotil) also has atropine to inhibit secretion

131
Q

What is the effect of bismuth subsalicyclate

A

Inhibitor of SI secretion (think sub-sali-vate - less secretions)

132
Q

What are Kaolin, attapulgite, dioctahedral smectite

A

Antidiarrheal absorbents of uncertain efficacy; minerals absorb water for firmer feces but no change in water loss

133
Q

What patients should not get cisapride

A

Boxers! dysrhythmia (boxers have a lot of heart and a lot of pride)

134
Q

Why should antibiotics be avoided for the gut

A

Bacterial infections are rare and Abx destabilize normal flora

135
Q

What situations should antibiotics in GI issues be used

A

When sepsis is likely due to breakdown of mucosal barrier (parvo, chemo), sometimes in hemorrhagic diarrhea and prolonged starvation, and specific infections

136
Q

What antibiotics should be used in hemorrhagic diarrhea and prolonged starvation for the upper intestine

A

Gram + and -, first generation cephalosporins

137
Q

What antibiotics should be used in hemorrhagic diarrhea and prolonged starvation for the lower intestine

A

Combo gram negative and anaerobes

138
Q

What should be used for salmonella and acute pancreatitis

A

Enrofloxacin

139
Q

What should be used for boxer colitis and e. coli colonization

A

Enrofloxacin

140
Q

What should be used for clostridial colitis

A

Metronidazole

141
Q

In SI dysbiosis, which antibiotics should be used

A

Tetracycline, metronidazole, tylosin

142
Q

What organism is in Fortiflora

A

Enterococcus faecium

143
Q

What organism is in Prostora Max

A

Bifidobacterium animals (think FIDO and MAX as dog names)

144
Q

How should probiotics be used?

A

Every day because population is determined by food supply, so will be immediately eliminated if not

145
Q

How are oligisaccharides, beet pulp and soluble fiber used?

A

Pre-biotic carbohydrates not digested in SI

146
Q

What is the purpose of beet pulp

A

Prebiotic mixing soluble and insoluble fiber

147
Q

What methods can be used to control diarrhea

A

Contraction via morphine agonists, inhibitors of SI secretion, absorbents

148
Q

GI: What is the immunosuppressive dose of prednisone/solone

A

1-2mg/kg bid for 2-4 weeks

149
Q

What is the weaning recomendation for pred

A

Reduce by half every 2-3 weeks until every other day at low dose. Increase one step if signs occue

150
Q

What corticosteroid anti-inflammatory should be used if acites is present

A

Dexamethasone

151
Q

What kind of drug is budesonide?

A

corticosteroid

152
Q

Why is pred usually just used at antiinflammatory doses?

A

Bc leukotriene inhibitors are more effective than PG inhibitors like pred

153
Q

What is the metabolism of budesonide

A

First pass through liver - so less side effects than prednisone

154
Q

What kind of drugs are azathioprine, cyclophosphamide, chlorambucil?

A

Alkylating agents for anti-inflam/immuno

155
Q

What is azathioprine used for

A

lowering long term pred use

156
Q

How should azathioprine be given

A

To lower long term pred use: One month to work, so give for three months SID then EOD

157
Q

What precautions should be taken with azathioprine?

A

Monitor WBC count

158
Q

What kind of drug is cyclophosphamide?

A

alkylating agent for antiinflamm/immunosuppressive

159
Q

What are the benefits of cyclophosphamide

A

Rapid onset compared to azathioprine

160
Q

What are the possible side effects of cyclophosphamide

A

Hemorrhagic cystitis, neutropenia

161
Q

What type of drug is chlorambucil

A

Alkylating agent for antiinflammation and immunosuppression

162
Q

What drug should be used for small cell lymphoma and IBD

A

Chlorambucil

163
Q

What kind of drug is cyclosporine and what is its action

A

Anti-inflammation/immune suppressive- modifies cell mediated immunity

164
Q

What drug should be used for anal fistulas

A

Cyclosporine

165
Q

How can dose of cyclosporine be lowered

A

Give with ketoconazole

166
Q

What is the effect and mechanism of leflunomide

A

Suppression of T cell function by inhibiting pyrimadine synthesis

167
Q

What is the effect of mycophenolate mofetil

A

Suppression of T cells function by inhibiting purine synthesis

168
Q

What are the osmotic agents that can be used as laxatives

A

Magnesium sulfate (epsom salts) and Colyte

169
Q

What drug should be used before a colonoscopy

A

Colyte

170
Q

What are the bulk forming osmotic agents that can act as laxatives

A

Insoluble fiber; Soluble fibers: methylcellulose, psyllium, and pumpkin; Indigestible sugars: lactulose

171
Q

What kind of drug is magnesium sulfate?

A

Epsom salts: osmotic agent laxative

172
Q

What laxative should be used in cats

A

Pumpkin

173
Q

What lubricants can be used as laxatives

A

mineral oil, petrolatum

174
Q

What kind of drug is petrolatum

A

Lubricant laxative- Laxitone!

175
Q

Name the drugs that can be used to treat whip worms

A

Fenbendazole (panacur), febantel (drontal), moxidectin (adv. multi), milbemycin (trifexis)

176
Q

What caution should be taken with mineral oil

A

risk of inhalation pneumonia

177
Q

Why should phsphate fleet enemas be avoided?

A

Can cause toxicity hypophosphatemia

178
Q

What is a possible side effect of bismuth subsalicylate

A

Peptobismol- can cause black feces from the bismuth

179
Q

What are the risks of sulfasalazine?

A

Risk of dry eye autoimmune disease

180
Q

What is a good alternative to sulfasalazine?

A

Olsalazine - lower side effects but very expensive

181
Q

What kind of drug is sulfasalazine?

A

Aminosalicylate anti-inflammatory to treat colitis

182
Q

When should prophylactic antibiotics be used

A

20-30 minutes before surgery, q 90 minutes after

183
Q

Which antibiotic is best for pre-sx

A

Cefazolin

184
Q

What is Cmax

A

Maximum serum concentration of a drug

185
Q

What is MIC

A

Minimum inhibitory concentration

186
Q

Cmax/MIC ratio- what should be high/low

A

Cmax high, MIC low

187
Q

What is AUC

A

Area under the curve for plasma concentration

188
Q

*****What is AUC24/MIC

A

Ratio of area under the plasma concentration time curve for a 24 hour interval to the MIC

189
Q

What is T>MIC

A

The percentage of time during a dosing interval that a drug exceeds MIC

190
Q

What is Tmax

A

Time to maximum plasma concentration

191
Q

What is Cl total

A

Plasma clearance of a drug in a period of time- how fast it can be removed from the patient

192
Q

****What is AUC

A

The extent of drug absorption

193
Q

What effect does doubling a dose have on Cmax and T1/2

A

Doubles the Cmax and adds a half life, but doesnt change the length of the half life

194
Q

What does it mean to be concentration dependent

A

As concentration increases, efficacy also increases

195
Q

What Pk/Pd parameter relates to concentration dependent drugs

A

Cmax/MIC and AUC24/MIC

196
Q

Cmax/MIC and AUC24/MIC are parameters related to what Pk/Pd profile

A

Concentration dependent

197
Q

What does it mean to be time dependent?

A

Increases in dose will not change efficacy

198
Q

What Pk/Pd parameters relate to time dependent drugs with no persistent effects?

A

T>MIC

199
Q

T> MIC is a Pk/Pd parameter related to what profile?

A

Time dependent with no persistent effects

200
Q

What is the goal of therapy with concentration dependent drugs

A

Maximize concentration

201
Q

What is the goal of therapy with time dependent, no persistent effects drugs

A

Maximize duration of exposure

202
Q

What is the goal of therapy with time dependent, with persistent effects drugs

A

Maximize the amount of the drug

203
Q

What Pk/Pd parameter is related to time dependent, with persistent effects drugs

A

AUC24/MIC

204
Q

AUC24/MIC is a Pk/Pd parameter for which profile

A

time dependent, with persistent effects drugs

205
Q

For concentration dependent drugs, Cmax should be

A

8-10 times MIC

206
Q

How long should the inter-dosing interval exceed MIC in drugs like penicillin

A

30-50%

Pharmacology Test Two (6 decks)

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