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Pharm > CPEE TEST 1 > Flashcards

CPEE TEST 1 Flashcards

1
Q

Somatropin

A
  • 191 AA GH analog
  • Given 3-7/week SC or IM
  • Activate GH receptor –> Jak-Stat Pathway
  • Children with GH deficiency prior to epiphysial closure
  • Doesn’t work in Laron form of dwarfism due to GH receptor defect
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2
Q

Sermorelin

A
  • GHRH analog (1-29 AA residues, increase t 1/2)
  • IV, SC, Nasal
  • Activates GHRH receptor –> GH release –> IGF-1 release
  • GH analog preferred
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3
Q

Mecasermin

A
  • IGF-1 Analog
  • Laron Dwarfism
  • Hypoglycemia, Overgrowth of facial bones, antibodies may lead to resistance
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4
Q

Octreotide

A
  • Synthetic Analog of somatotropin (8-AA cyclic peptide, stabilized)
  • Longer T-1/2 and less decrease of insulin secretion
  • 2-3 injections/day
  • Treat acromegaly due to GH secreting tumor or hormone secreting tumors with SST receptors
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5
Q

Pegvisomart

A
  • GH receptor antagonist

- Used to treat Acromegaly.

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6
Q

Prolactin System

A

-Release stimulated by TRH and inhibited by Dopamine

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7
Q

Cabergoline

A
  • DA agonist analog to inhibit PRL release
  • Orally effective 1-2/week
  • PRL inhibition is via D2 receptor and Cabergoline is D2 selective
  • Treat hyperprolactinemia, prolactinoma, suppression of lactation, inhibit GH release (acromegaly)
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8
Q

Arginine Vasopressin

A
  • ADH analog short acting
  • IV, IM, SC
  • V1 (vasoconstriction) and V2 (aquaporin channels and von willebrand factor) effects.
  • Choice for V1 applications
  • Treatment of temporary diabetes insipidus
  • CV: Local admin for constriction, Vasoconstriction in resuscitation of V tach or V fib
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9
Q

Desmopressin Acetate

A
  • Modified synthetic analog of ADH
  • Longer acting and more V2 action
  • First orally available peptide
  • First choice diabetes insipidus
  • Caution with overnight use –> hyponatremia
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10
Q

Drugs used to INCREASE TH

A

Levothyroxine and Liothyronine

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11
Q

Levothyroxine

A
  • Pure T4 with slow onset, but long duration
  • Primary drug used in hypothyroidism due to long duration
  • IV form used for Myxedema coma
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12
Q

Liothyronine

A

-Used mostly to maintain suppressive effects of TH on TSH prior to surgery thyroid cancer

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13
Q

Use of TH in older patients or patients with Cardiac disease

A

-Start small and slowly increase b/c increase metabolic demand can strain weakened hearts

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14
Q

TH hormone use in Myxedema Coma

A

-Levothyroxine IV initially followed by oral maintenance

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15
Q

Drugs used to treat HYPERTHYROIDISM

A
  • Propanolol
  • Thioamide (Propyluracil and methimazole) to block synthesis of T4
  • Radioiodine to destroy thyroid.
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16
Q

Methimazole and Propylthiouracil: MOA, Uses, Pharmacokinetics, and Adverse effects

A

Inhibit Peroxidase, iodination, coupling, and block synthesis. DON’T inhibit release of preformed TH

  • Used for first line therapy of hyperthyroidism
  • Well absorbed orally and concentrated in thyroid so duration of action is longer than plasma half life.
  • Agranulocytosis occurs, but rare. If person has sore throat and fever in the first few months of therapy stop and give antibiotics
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17
Q

Propylthiouracil

A
  • Less potent and short half-life
  • Preferred in THYROID STORM because it blocks T4 –> T3 conversion
  • Also preferred in pregnancy due to lack of side effects (Generally treat to moderately hyperthyroid status
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18
Q

Methimazole

A
  • more POTENT and longer acting than propylthiouracil

- Doesn’t cause liver toxicity/failure

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19
Q

Potassium Iodide

A
  • Inhibits synthesis and release of TH
  • Rapid effects, but short duration.
  • Decreases vascularization and firms up gland prior to surgery
  • Beneficial in THYROID STORM to stop release of preformed hormone
  • Radiation emergencies to prevent uptake of radioactive iodine
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20
Q

Regular Insulin

A

Physiologic level of zinc and no protein added

  • Short acting
  • Onset 30-1 hr, Peak 2-4, duration, 5-8
  • IV
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21
Q

Isophane insulin suspension

A
  • Complex with protein at neutral pH
  • Slower absorption and longer action than reg. insulin
  • Cloudy suspension CAN’T be given IV
  • Between meals
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22
Q

Insulin Lispro

A
  • Analog
  • Lys 28 Pro 29 (Normally opposite)
  • Less aggregation –> Faster absorption
  • Shorter Action
  • Peak 30-60 w duration of 3-4 hrs
  • Can be injected immediately before meals
  • IV
  • Less danger of hypoglycemia due to dosage close to meals
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23
Q

Insulin Aspart

A
  • Pro 28 replaced with Asp
  • Similar to Lispro but longer duration of action (between regular and lispro)
  • Injected at meal times and CAN be given IV
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24
Q

Insulin Glulisine

A
  • Lys 29 replaced by Glu and Asp 3 replaced by Lys
  • Injected before or immediately after meal.
  • IV
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25
Q

Insulin Glargine

A
  • Gly 21 in A chain and 2 Arg added at C-terminus of B chain
  • W/ Zn @ pH 4 to decrease aggregation
  • Forms hexamers that precipitate at site of injection
  • SC administration once per day
  • DONT mix with other insulins in the same syringe
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26
Q

Insulin Detemir

A
  • Similar kinetics to Glargine
  • Thr 30 deleted and myristic acid chain added to Lys 29
  • Binds to albumin via fatty acid chain
  • Better and Less variable absorption than Glargine
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27
Q

Pramlintide

A
  • Analog of Amylin which is released from Beta cells with insulin
  • Decreases post prandial glucose, liver glucose production and slows gastric emptying
  • Type 1 and 2 Diabetics who lack control with insulin alone
  • Injected SC before meals
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28
Q

Glucagon

A

Counter regulatory to insulin.

  • Used with hypoglycemia
  • IM or SC
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29
Q

Diazoxide

A

-Opens ATP sensitive K+ channels to inhibit glucose release

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30
Q

Prototype Sulfonylurea

A

-Glimepiride

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31
Q

Sulfonylureas: MOA and PK

A
  • Closes ATP sensitive K+ –> insulin release and increase tissue sensitivity to insulin and decrease glucagon
  • Well absorbed orally, protein bound, liver metabolism w/ kidney excretion (Once daily)
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32
Q

Sulfonylureas: Side effects

A
  • HYPOGLYCEMIA especially when used with insulin
  • WEIGHT GAIN
  • Dont use in patients with LIVER or KIDNEY DISEASE
  • Falling out of favor
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33
Q

Meglitinide prototypic drug

A

Repaglinide

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34
Q

Meglitinide (Repaglinide) MOA, PK

A
  • MOA: Similar mechanism to Glimepiride, closes K+ channels Lowest effects of all oral agents
  • Faster than SU (glimepiride) but shorter duration
  • 30 min before meal
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35
Q

Meglitinide (Repaglinide) Side effects

A
  • HYPOGLYCEMIA
  • WEIGHT GAIN
  • MAY be safer than SUs in kidney disease
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36
Q

Biguanide Prototypic drug

A

METFORMIN BABY!

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37
Q

Biguanide (Metformin): MOA, Uses

A
  • Primary effects in liver: decreases glucose production and increases uptake, and increases insulin effectiveness
  • DOESN’T increase insulin secretion
  • Upstream action on AMP kinase pathway (regulates glucose metabolism)
  • Used with insulin to make insulin more effective
  • 1ST LINE DRUG AGAINST DIABETES
  • CAN BE USED WITH SUs AND OTHER ORAL AGENTS
38
Q

Biguanides (Metformin): PK and Side effects

A
  • Orally effective typically 2-4 times per day w/meals, ER available
  • Renal excretion (KIDNEY DISEASE)
  • Inhibits lactic acid metabolism (LIVER DISEASE)
  • NO HYPOGLYCEMIA
  • NO WEIGHT GAIN
  • Inhibits lactate metabolism
39
Q

Alpha Glucosidase Inhibitors

A

-Miglitol and Acarbose

40
Q

Alpha Glucosidase Inhibitors (Miglitol and Acarbose): MOA and PK

A
  • Microbial sugars that inhibit mammalian sugar metabolizing enzymes
  • Immediately before meal
  • NOT POWERFUL
  • Used with insulin or other oral agents
  • Acarbose = Complex = longer in gut
  • Miglitol= Simple monosacchride = absorbed
41
Q

Alpha glucosidase inhibitors (Miglitol and Acarbose): Side Effects

A
  • HYPOGLYCEMIA w/ insulin/OA (Must use glucose to treat)
  • Flatulence
  • Avoid with Metformin
42
Q

Thiazolidinediones (Pioglitazone and Rosiglitazone): MOA

A
  • Bind to PPAR-Gamma, nuclear transcription factor –> ^transcription of insulin responsive genes (make insulin more effective)
  • Also use AMP Kinase like Metformin
  • Decrease: Gluconeogenesis, glucose output and triglyceride synthesis in liver
  • Increase Glucose uptake and utilization in muscle
  • Most often used with insulin, SU and/or Metformin
43
Q

Thiazolidinediones (Pioglitazone and Rosiglitazone): PK

A
  • Orally effective best with food once daily

- Metabolized in LIVER and excreted in FECES

44
Q

Thiazolindinediones (Pioglitazone and Rosiglitazone): Side effects

A
  • Hepatotoxicity and fatal liver disease

- NO HYPOGLYCEMIA

45
Q

GLP-1 Agonist (Exenatide): Effects and Uses

A
  • GLP-1 Analog
  • Increases insulin secretion
  • Slows gastric emptying
  • Reduces post prandial glucose
  • LACK OF WEIGHT GAIN (weight loss)
  • Metformin/SU/Insulin Glargine for Type 2 (SC before meals
46
Q

GLP-1 Agonist analog (Exenatide): Side Effects

A
  • HYPOGLYCEMIA with SU
  • Renal Failure risk
  • Take antibiotics and Contraceptives before because of altered absorption.
47
Q

DPP-IV Inhibitor (Stiagliptin): Mechanism, PK, and Uses

A
  • Inhibits DPP-IV which degrades GLP-1
  • Orally once/day
  • Monotherapy
  • Use with Meformin (Biguanide) or Rosiglitazone (Thiazolidinedione)
  • NO WEIGHT GAIN OR HYPOGLYCEMIA
48
Q

SLGT-2 Inhibitors (Canagliflozin): MOA and Side effects

A
  • Inhibits SLGT2 that mediates reentry of glucose in to kidney –> More glucose excretion in the urine
  • Orally once per day
  • Increased risk of urinary tract infections
49
Q

Hydrocortisone

A
  • Active at both GC and MC receptors
  • Orally effective
  • Adequate for most endocrine uses
  • Many OTC preparations for inflammation
50
Q

Prednisone

A
  • More potent due to slower metabolism

- Partially selective for GC vs MC (uses in inflammation)

51
Q

Dexamethasone & Betamethasone

A
  • Highly GC selective
  • Very long duration of action
  • Very potent (decrease protein binding and mods that slow metabolism)
  • Very strong GC effects w/ no MC effects
  • Used for inflammation if high doses of
  • Bethamethasone used to increase surfactant production in infants.
52
Q

Fludrocortisone

A
  • Increased potency and activity at MC receptor w strong GC activity
  • Once per day
  • MC replacement therapy or action
53
Q

COX-1

A
  • Fever and Pain

- Increase platelet aggregation

54
Q

COX-2

A
  • Pain and inflammation

- Decreased endothelial aggregation

55
Q

Metabolism of Salicylate

A
  • Low doses: liver by conjugation (first order/saturable)

- Higher does: unmetabolized and excreted via the kidneys (zero-order)

56
Q

Doses for inhibition of inflammation, analgesic, and anti pyretic effects

A

Inflammation: higher doses that saturate liver and renal elimination (COX-2)
Analgesic and anti-pyretic: lower doses (COX-1)

57
Q

Aspirin effects to prevent thrombus and prolong bleeding time

A
  • COX-1: make thromboxanes which increase clotting so want supression (low dose)
  • COX-2: Make prostacyclins which decrease clotting and thrombosis risk (need a higher dose to inhibit, but don’t want to inhibit)
58
Q

Propionic Acid Derivatives

A

Ibuprofen and Naproxen

59
Q

Ibuprofen and Naproxen

A
  • Reversible and competitive inhibition of COX

- Bind heavily to albumin (displace warfarin)

60
Q

Ibuprofen

A
  • Low dose for analgesia and antipyresis
  • High dose for anti-inflammation
  • Can block effects of low dose aspirin
61
Q

Naproxen

A

-Higher doses with prescription

62
Q

Acetic Acid Derivatives

A

-Indomethacin, Celecoxib, and acetaminophen

63
Q

Indomethacin

A
  • 20 times more potent than asprin

- Mainly used for severe inflammation

64
Q

Celecoxib

A
  • Selective COX-2 Inhibitor
  • Treat inflammation and avoid COX-1 side effects
  • Osteo and rheumatoid arthritis
  • Fewer problems in asthmatics
  • Increased risk of MI (clotting)
  • Edema b/c decreases kidney function
65
Q

Acetaminophen

A
  • NO anti-inflammatory action
  • Doesn’t really have any of the side effects that aspirin has
  • cross sensitivity with aspirin can be serious
  • Hepatic damage with alcohol (due to to reactive electrophile metabolites that can modify liver proteins
66
Q

N-Acetylcysteine

A

-Sulfhydryl compound to capture reactive acetaminophen or replace glutathione levels jhfgj

67
Q

Mu Receptors

A
  • Morphine like actions
  • CNS spinal cord and periphery
  • analgesic, anti-anxiety, resp depression, euphoria, physical dependence, GI, and sedation
68
Q

Kappa Receptors

A
  • Pentazocine like actions
  • CNS and spinal cord
  • Analgesia, miosis, sedation, dependence, dysphoria, and Hallucinations
69
Q

Delta Receptors

A
  • Enkephalin like actions
  • CNS periphery
  • Dependence, euphoria, analgesia
70
Q

Enkephalins

A

-Act at delta and mu receptors

71
Q

Dynorphins

A
  • Act at Mu and Kappa

- opiate receptor agonists longer acting than enkephalins

72
Q

Endorphins

A

-Act at Kappa, Mu, and Delta receptors

73
Q

Morphine

A

Natural constituent of opium

  • Absorbed by all routes, EtOH can break down slow release matrix
  • Conjugation with glucuronic acid in liver (morphine-3-beta-glucuronide can induce seizures)
  • Develop tolerance
74
Q

Morphine Analgesia

A
  • Blocks peripheral and spinal transmission of pain and blocks response to pain
  • More effective against continuous dull pain
  • Raising pain threshold and anti-anxiety effect important for severe pain
75
Q

Morphine Respiratory depression

A
  • Primary cause of death in overdose
  • decreases chemoreceptor sensitivity to CO2 but Hypoxia response still present
  • FOR ALL OPIODS THE GIVEN RESPIRATORY DEPRESSION AT A GIVEN LEVEL OF ANALGESIA IS THE SAME
76
Q

Morphine naseau and vomiting

A

-stimulation of chemoreceptor, tolerance develops quickly

77
Q

Morphine and GI effects

A

-Constipation, no tolerance develops

78
Q

Morphine and pupilary constriction

A

-No tolerance, diagnostic

79
Q

Morphine Limitation and Contraindications

A
  • Decreased respiratory reserves
  • Head injuries
  • Pregnancy
  • Don’t use with CNS depressant
80
Q

Codeine

A
  • More reliable orally compared to morphine
  • Mild to moderate pain
  • Effective for cough suppression
  • More constipation
81
Q

Methadone

A
  • Very effective orally
  • CYP3A4
  • T1/2 of 15 hrs
  • Serious CV effects
  • Parenteral euphoria and dependence
  • Analgesia and treatment of drug dependence
82
Q

Fentanyl

A
  • Extremely potent opioid agonist
  • Treats chronic (patch) and breakthrough pain (nasal spray or tablet)
  • similar effects to morphine
  • Muscle rigidity of
83
Q

Hydrocodone

A

-most prescribed drug

84
Q

Oxycodone

A

More potent than hydros

85
Q

-Loperamide

A

-Potent anti-diarrheal agent full opioid agonist action limited to GI tract

86
Q

Dextromethorphan

A
  • Cough supressant

- No analgesia

87
Q

Partial opioid agonist

A
  • agonists when given alone
  • most kappa receptors
  • limited analgesic and respiratory depression effects
  • Antagonists when on board with full agonist
  • Pentazocine
  • Buprenorphine
  • Tramadol
88
Q

Pentazocine

A
  • similar to morphine
  • Kappa partial agonist
  • mu antagonist/partial agonists
  • analgesia sedation and resp depression, similar to morphine at normal doses
  • dysphoria at high dose
  • may precipitate withdrawal in opioid dependent people due to antagonist action
  • analgesia in moderate to severe pain
89
Q

Buprenorphine

A
  • partial agonist at mu receptors
  • antagonist at kappa receptors
  • analgesia in moderate to severe pain (has a ceiling)
  • similar effects to morphine on eyes and gi tract
  • uses analgesia and treatment of opioid dependence
90
Q

Tramadol

A
  • Weak mu agonist
  • can produce dependence
  • Inhibits NE and 5HT transport
  • seizures serotonin syndrome
91
Q

Opioid antagonists

A

-Naloxone

92
Q

Naloxone

A
  • opioid antagonist with no agonist actions at normal doses
  • used to counteract effects of opioids
  • will precipitate withdrawal

Pharm (8 decks)

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