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Exam III Flashcards

1
Q

Sodium Bicarbonate

A
  • aka Alka Seltzer
  • antacid = neutralizes gastric acid.
  • fast acting, short duration
  • CO2 ⇒ belching, flatulence
  • only used short term, not very effective
  • use: heart burn
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2
Q

Calcium Carbonate

A
  • aka Tums
  • antacid = neutralizes gastric acid
  • fast acting, short duration.
  • CO2 ⇒ belching, flatulence
  • only used short term, not very effective
  • causes rebound ↑ H+ secretion
  • use: heart burn
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3
Q

Magnesium Hydroxide

A
  • antacid
  • given in combo with Aluminum Hydroxide
  • alone causes diarrhea (saline laxative)
  • toxicity in pts with renal insufficiency
  • use: heart burn, acute constpipation
  • side effects: hypermagnesemia in pts with renal insufficiency
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4
Q

Aluminum Hydroxide

A
  • antacid
  • given in combo with magnesium hydroxide
  • alone causes constipation
  • toxicity in pts with renal insufficiency
  • use: heart burn
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5
Q

Antacids

A
  • neutralizes gastric acid
  • fast acting, short duration
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6
Q

PPI

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
    • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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7
Q

H2 Blockers

A
  • reduce gastric acid secretion
  • faster onset than PPI but less effective
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding in the critically ill (stress gastritis)
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8
Q

Gastrin

A
  • acts on parietal cells, enterochromaffin-like cells (ECL)
  • parietal cells: stimulates H+K+ ATPase (proton pump) via CCK2 receptor ⇒ gastric acid release
  • ECL: stimulates release of histamine ⇒ parietal cell activation
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9
Q

Histamine

A
  • acts on parietal cells
  • via H2 receptor, stimulates H+K+ ATPase ⇒ gastric acid release.
  • causes: bronchoconstriction, ↑ GI motility, ↑ gastric acid, ↑ HR, vasodilation, pain and itching, triple response (reddening, wheal, flare)
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10
Q

ACh (GI)

A
  • acts on parietal cell and enterochromaffin like cell (ECL)
  • parietal: thru M3 stimulates H+K+ ATPase ⇒ gastric acid release
  • ECL: release histamine ⇒ parietal cell activation
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11
Q

Omeprazole

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
    • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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12
Q

Esomeprazole

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
  • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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13
Q

Lansoprazole

A
  • inhibits H+K+ ATPase
  • reduce gastric acid secretion
  • long acting, take 1x a day
  • prodrug, take 1 hr before eating (take on empty stomach, is weak base)
  • t1/2 = <2hr, hepatic elimination
  • 3-4 days for max effect
  • converted to active form in stomach
  • use: GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding.
    • H. pylori: use PPI with 2 antibiotics
  • side effects: ↑ risk GI infection
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14
Q

Cimetidine

A
  • H2 blocker
  • faster onset than PPI but less effective
  • use: heart burn (dydpepsia), GERD, peptic/duodenal ulcers, prevent NSAID ulcers, prevent stomach bleeding in critically ill (stress gastritis)
  • side effects: drug interactions (inhibits CYP)
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15
Q

Ranitidine

A
  • H2 blocker
  • faster onset than PPI, less effective
  • reduces gastric acid secretion
  • use: heart burn, GERD, peptic/duodenal ulcers, prevent NSAID ulcers, stress gastritis in critically ill
  • side effects: well tolerated
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16
Q

Famotidine

A
  • H2 blocker
  • reduces gastric acid secretion
  • faster onset than PPI but less effective
  • use: heart burn, GERD, peptic/duodenal ulcers, prevent NSAID ulcers, stress gastritis in critically ill
  • side effects: well tolerated
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17
Q

Sucralfate

A
  • mucosal protective agent
  • slurry dose, use QID via NG tube
  • use: stress-related gastritis
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18
Q

Misoprostol

A
  • mucosal protective agent
  • PGE1 analog
  • QID orally
  • use: prevent NSAID ulcers
    • use with antipregestin to expel aborted fetus
  • side effects: diarrhea, abd cramps/pain
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19
Q

Bismuth-Salicylate

A
  • aka Peptobismol
  • use: dyspepsia, diarrhea, in 2nd line therapy for H pylori
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20
Q

Metoclopramide

A
  • D2 blockade, 5-HT4 agonism, 5-HT3 antagonism
  • suppresses DA effects on ACh release from myenteric plexus ⇒ ↑ stomach emptying, ↑ upper GI motility
  • D2 block ⇒ ↓ nausea/vomiting from chemo trigger zone
  • use: ↑ stomach emptying in diabetic/post surg gastric stasis, GERD resistant to PPI/H2 blockers, anti-emetic, CINV**
  • side effects: sedation, restlessness, anxiety, agitation in elderly, extra-pyramidal symptoms, irreversible tardive dyskinesia
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21
Q

Erythromycin

A
  • macrolide antibiotic
  • stimulates GI motility via motilin
  • use: gastric stasis
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22
Q

Methylnatrexone

A
  • opioid antagonist
  • doesn’t cross BBB
  • use: prevent opioid induced constipation without blocking analgesia
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23
Q

Alvimopan

A
  • opioid antagonist
  • can’t cross BBB
  • use: prevent opioid induced constipation without blocking analgesia
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24
Q

Stimulant Laxatives

A
  • act on enteric nerves to ↑ colon contractions and secretions
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25
Bisacodyl
* **stimulant laxative** * acts on enteric nerve to ↑ colon contractions and secretions * 6-10 hr onset after oral, 30-60 min rectal onset * _use_: **with stool softeners to prevent/treat opioid constipation, with osmotic laxative before bowel surgery/exam**
26
Anthraquinones
* stimulant laxatives * 6-12 hr onset orally, 2 hr rectally * not safe
27
Osmotic Laxatives
* poorly absorbed * retain water in GI tract via osmotic activity
28
Balanced Polyethylene Glycol Solution
* **osmotic laxative** * retain water in GI tract via osmotic activity * _use_: **bowel cleansing before exams\*\***, prevent/treat constipation
29
Saline Laxatives
* magnesium or phosphate salts * fast acting
30
Sodium Phosphate
* **saline laxative** * fast acting 1-3 hr * _use_: **two dose regiment for bowel cleansing before exams** * dont' use in pts with renal/cardiac disease, electrolyte abnormalities
31
Magnesium Citrate
* **saline laxative** * _use_: **acute constipation** * _side effect_: **hypermagnesemia in pt with renal insufficiency**
32
Lactulose
* **indigestible sugar** * converted to fatty acids by colonic bacteria ⇒ acid trap ⇒ **↓ blood ammonia in hepatic encephalopathy** * slow acting 24-48 hr * _side effect_: **flatulence, cramps**
33
Sorbitol
* **indigestible sugar** * slow acting 24-48 hr * induces diarrhea * _side effect_: **flatulence, cramps**
34
Mannitol
* **indigestible sugar/alcohol** * slow acting 24-48 hr * induces diarrhea * _side effect_: **flatulence, cramps**
35
Bulk Forming Laxatives
* slow acting 1-3 days * **absorbs water, distends colon, promotes peristalsis**.
36
Bran
* bulk-forming laxative * slow acting 1-3 days * absorbs water, **promotes peristalsis**
37
Psyllium
* **bulk-forming laxative** * slow acting 1-3 days * absorbs water, **promotes peristalsis**
38
Methylcellulose
* **bulk-forming laxative** * short acting 1-3 days * absorbs water, **promotes peristalsis**
39
Polycarbophil
* **bulk-forming laxative** * slow acting 1-3 days * absorb water, **promote peristalsis**
40
Stool Softeners
* slow acting 1-3 days * increase water and lipid content in stool * give oral or rectal
41
Docusate
* **stool softener** * slow acting 1-3 day * **increases water and lipid** in stool
42
Lubiprostone
* **chloride channel activator** * prostanoic acid analog * **increases intestinal secretions** * _use_: **chronic constipation, IBS with constipation**
43
Loperamide
* **meperidine analog** * _use_: OTC for **diarrhea**
44
Simethicone
* anti-foaming agent * _use_: **reduce esophageal reflux** when with antacids
45
Ocreotide
* **somatostatin** analog * **inhibits secretion of GI/pancreatic hormones and 5-HT** * use: **dumping syndrome/diarrhea after gastric surgery; watery diarrhea and flushing etc from carcinoid tumors and VIPomas; ↓ portal pressure and variceal bleeding from chronic liver disease**
46
Alosetran
* **long acting 5-HT3 antagonist** * _use_: **IBS with diarrhea** * _side effects_: **constipation, fatal ischemic colitis**
47
Vomiting Center Stimulants
* from chemoreceptor trigger zone: D2, opioid, NK1, 5-HT3 * vestribular system: M1, H1 * vagal and spinal afferents: 5-HT3
48
-setron
* **5-HT3 antagonists** * no drug interactions * _use_: **nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV**
49
Odansetron
* **5-HT3 antagonist** * no drug interactions * _use_: **nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV**
50
Granisetron
* **5-HT3 antagonist** * no drug interactions * _use_: **nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV**
51
Dolasetron
* **5-HT3 antagonist** * no drug interactions * _use_: **nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV**
52
Palosetron
* **5-HT3 antagonist** * longest t1/2 * no drug interactions * _use_: **nausea and vomiting; with dexamethosome for acute CINV; with NK1 antagonist for delayed CINV**
53
Dexamethosone
* **corticosteroid** * oral or IV * **enhances effects of 5-HT3 antagonists** * _use_: **with 5-HT3 antagonists for CINV**
54
NK1 Antagonist
* **antagonizes substance P in periphery and CNS** * **enhances effects of 5-HT3 antagonists** * may **inhibit** drug metabolism by **CYP3A4** * _use_: **with 5-HT3 and dexamethosone for delayed CINV**
55
Aprepitant
* **NK1 antagonist** * **antagonizes substance P in periphery and CNS** * **enhances effects of 5-HT3 antagonists** * may **inhibit **drug metabolism by **CYP3A4** * _use_: **with 5-HT3 and dexamethosone for delayed CINV**
56
Fosaprepitant
* **NK1 antagonist** * **antagonizes substance P in periphery and CNS** * **enhances effects of 5-HT3 antagonists** * may **inhibit **drug metabolism by **CYP3A4** * _use_: **with 5-HT3 and dexamethosone for delayed CINV**
57
Droperidol
* **cannabinoid** * **strong D2 blocking effects** * _use_: **CINV** * _side effect:_ **QT prolongation and sudden death**
58
Cyclizine
* H1 antagonist * use: motion sickness
59
Scopolamine
* antimuscarinic * use: motion sickness
60
Benzos
* anxiolytic * _use_: **reduce anticipatory nausea and vomiting with chemo**
61
Pancrelipase
* pancreatic extract **containing lipase, amylase, proteolytic activity** * take before meals * _use_: **pancreatic enzyme deficiency from cystic fibrosis, pancreatitis**
62
Ursodiol
* natural bile acid * _use_: **dissolve small cholesterol gallstones, prevent gall stones during rapid weight loss, treat cholesterol gallstones as last resort**
63
**5-ASA**
* 5-amilosalicylic acid * **anti-inflammatory** on diseased GI mucosa. * _use_: **induce/maintain remission in mild-mod UC, Crohn's**
64
Basalazide
* **5-ASA analog with azo linkage** * converted in gut to 5-ASA * _use_: **IBD**
65
Olsalazine
* **5-ASA analog with azo linkage** * converted in gut to 5-ASA * _use_: **IBD**
66
Sulfasalazine
* **5-ASA analog with azo linkage** * converted in gut to 5-ASA * _use_: **IBD** * not well tolerated
67
Mesalamine
* 5-ASA delayed release tablets, enemas, and suppositories
68
Budesonide
* **glucocorticoid** * _use_: **IBD**
69
Azothioprine
* **antimetabolite** * anti-cancer drug **interferes with nucleotide synthesis.** * **inhibits cell proliferation**, immunosuppressive effect * _use_: **low dose for IBD, induce/maintain remission of UC and Crohn's**
70
6-Mercaptopurine
* **antimetabolite** * anti-cancer drug **interferes with nucleotide synthesis.** * **inhibits cell proliferation**, immunosuppressive effect * _use_: **low dose for IBD, induce/maintain remission in UC and Crohn's**
71
Inflixumab
* **TNFalpha Ab** * immunosuppressive * _use_: **mod-severe IBD** that doesn't respond to others
72
Adalimumab
* **TNFalpha Ab** * immunosuppressive * _use_: **mod-severe IBD** that doesn't respond to others
73
Certolizumab
* **TNFalpha Ab** * immunosuppressive * _use_: **mod-severe IBD** that doesn't respond to others
74
Natalizumab
* **anti-integrin Ab** * against **alpha4 subunit** of integrins * **interferes with leukocyte adherence and migration** thru vascular endothelium to GI mucosa target cells * _use_: **severe Crohn's** resistant to others * _side effect_: **fatal leukoencephalopathy** with latent JC virus
75
Delayed CINV
* \>24 hr after cancer therapy * due to GI mucosal damage triggering mociceptive input and release of 5-HT and mediators
76
Acute CINV
* \<2 hr after cancer therapy * from chemoreceptor trigger zone stimulation
77
H1
* causes ↑ Ca via Gq * in endothelial cells and smooth muscle * in lungs, GI, uterus, small blood vessels * constricts smooth muscle * dilates endothelial cells * ⇒ **bronchoconstriction, ↑ GI motility, ↑ uterine contraction, arterial vasodilation, venous vasoconstriction**
78
H2
* causes **↑ cAMP** via Gs * in **heart, stomach, mast cells, brain** * causes **↑ HR**
79
H3
* causes **↓ cAMP, activated ERK** * on **presynatpic membrane** * causes negative feedback
80
H4
* causes **↓ cAMP, ↑ Ca** * on **leukocytes** * in immune system, **regulates cytokine production**
81
H1 antagonists
* **1st gen cause sedation**, can cross BBB * 2nd gen don't cause sedation * _use_: **allergic rxn, motion sickness, Meniere's disease, sedation** * has **antiparkinson effects, anticholinergic effects, antiserotinergic effects, local anesthesia via inhibited voltage gated Na channels, orthostatic hypotension**
82
Chlorpheniramine
* **1st gen H1 antagonist** * causes sedation * use: **allergic rxn, motion sickness, Meniere's disease, sedation**.
83
Diphenhydramine
* **1st gen H1 antagonist** * causes sedation * _use_: **allergic rxn, motion sickness, Meniere's disease, sedation**.
84
Pyrilamine
* **1st gen H1 antagonist** * causes sedation * _use_: **allergic rxn, motion sickness, Meniere's disease, sedation.**
85
Promethazine
* **1st gen H1 antagonist** * causes sedation * _use_: **allergic rxn, motion sickness, Meniere's disease, sedation**.
86
Cyproheptadine
* **1st gen H1 antagonist, 5-HT2 antagonist** * causes sedation * _use_: **allergic rxn, motion sickness, Meniere's disease, sedation, post gastrectomy dump syndrome**
87
Fexofenadine
* **2nd gen H1 antagonist** * _use_: **allergic rxn, motion sickness, Meniere's disease**
88
Loratadine
* **2nd gen H1 antagonist** * _use_: **allergic rxn, motion sickness, Meniere's disease**
89
Cetirizine
* **2nd gen H1 antagonist** * _use_: **allergic rxn, motion sickness, Meniere's disease**
90
Acrivastine
* **2nd gen H1 antagonist** * _use_**: allergic rxn, motion sickness, Meniere's disease**
91
5-HTR1
* causes ↓ cAMP via Gs
92
5-HTR2
* causes ↑ Ca via Gq * in periphery
93
5-HTR3
* works on ligand gated Na channel * not G protein coupled
94
5-HTR4
* causes ↑ cAMP via Gs
95
5-HTR6
* causes ↑ cAMP via Gs
96
5-HTR7
* ↑ cAMP via Gs
97
Buspirone
* anxiolytic * **5-HT1a agonist**
98
Sumatriptan
* **5-HT1d/1b agonist** * _use_: **migraines**
99
-triptan
* 5-HT agonists
100
Cisapride
* **5-HT4 agonist** * _use_: **gastroesophageal reflux**
101
Ritaserine
* 5-HT2R antagonist * reduces thromboxane formation * blocks DA reputake, improves mood in schizo
102
Ketaserin
* inhibits 5-HT2
103
5-HT
* acts as NT on H4 causing **↑ HR** * stimulates coronary bed * **pos chronotropic and inotropic effects** * triple response of BP: **↓ BP at outflow, ↑ BP in pulm and renal, ↓ BP in skeletal muscle** * causes **platelet aggregation** * **constricts smooth muscle in GI tract** (cause diarrhea and malnutrition)
104
'DONT' in Poisoning
* **Dextrose**: when altered mental status * from OD with insulin, insulin-secretagogues, slicylates, starvation * **Oxygen**: for hypoxia * **Naloxone**: for opioid overdose * **Thiamine**: for Wernike-Korsakoff syndrome, reduce ketoacidosis from starvation
105
Elevated Anion Gap in Poisoning
* causes **metabolic acidosis** * from toxic organic acid metabolites: **methanol, ethylene glycol** * from _lactic acidosis_: **salicylates in kids, cyanide in firefighters, CO**
106
Elevated Osmolar Gap in Poisoning
* with alcohols: ethanol, methanol, ethylene glycol
107
Hemodialysis in Poisoning
* for **salicylates, acetamiophen, methanol, ethylene glycol** * not for lipophilic drugs with low aqueous solubility or drugs with high Vd
108
Urinary Alkalinization in Poisoning
* to eliminate salicylates * not useful with rhabdomyolysis
109
Acetaminophen Antidote
* n-acetyl-l-cysteine
110
Toxic Alcohol Antidote
* ethanlol + fomepizole
111
CO Antidote
* oxygen
112
Cyanide Antidote
* hydroxocobalamin or nitrite + thiosulfate
113
Heroin Antidote
* naloxone
114
Iron Toxicity Antidote
* deferoxamine (chelates)
115
Inorganic Lead Antidote
* dimercaptrol, succimer, EDTA (chelators)
116
Mercury and Arsenic Antidote
* dimercaptrol, succimer
117
Anticholinesterase Antidote
* atropine, pralidoxime (for organophosphate ACHEI)
118
Salicylate Antidote
* bicarbonate
119
Cardiotoxic Drug Antidote
* bicarbonate
120
CO Poisoning
* causes hypoxia, headaches going to coma, death. * tx: oxygen
121
Salicylate Poisoning
* mild CNS: **hyperventilation, tinnitus, resp alkalosis ⇒ bicarb loss**. * sweating, nausea, vomiting ⇒ **dehydration** * severe poisoning (kids): **uncouples oxidative phosphorylation.** * **hyperthermia, metabolic acidosis, hypoglycemia, restlessness, delirium, seizures, depression, coma, resp and CV collapse, death.** * _tx_: **manage ABC, cool, give bicarb, give fluids, hemodialyze if severe**.
122
Acetaminophen OD
* causes liver failure * tx: gastric lavage, activated charcoal, N-acetylcysteine (NAC) to replenish glutathione and detoxify NAPQI
123
Serotonin Syndrome
* from SSRI, MAOI, amphetamines, meperidine, methadone, dextromethorphan * _mild symptoms_: anxiety, akathisia, tremors, tachycardia, sweating, diarrhea, mydriasis * _serotonin syndrome_: **clonus, hyper-vigilance, hyperthermia, HTN, hyperreflexia** * _severe_: **rigidity, hyperthermia \>40C, seizures, coma** * tx: discontinue drugs, give benzo anticonvulsants propranolol
124
Teratogens
* cytotoxic drugs * hormones * warfarin * methotrexate * ACEI, ARB
125
Isotretinoin
* synthetic retinoid * use: severe cystic acne * side effects: teratogen
126
Aciretin
* synthetic retinoid * use: psoriasis * _side effect_: **teratogen** (don't get pregnant for 3 yrs after stopping)
127
Mesolimbin DA Pathway
* mediates pleasure, euphoria, wanting, craving * causes withdrawal * to frontal cortex ⇒ learn cues for drug craving * to nucleus accumbens ⇒ wanting/craving
128
Acts on VTA
* VTA = ventral tegmental area in midbrain * acted on by ethanol, nicotine, opioids
129
Acts on Acc
* Acc = nucleus accumbens * acted on by cocaine, amphetamines, cannabinoids, opioids
130
Methadone
* maintenance of heroin addicts, opioids * reduces cravings, induces tolerance
131
Benzo (Drugs)
* for alcohol withdrawal and sedative hypnotics
132
Varenicline
* nicotinic receptor partial agonist * smoking cessation
133
Clonidine
* alpha 2 agonist * reduces SNS overactivity in opiate withdrawal
134
Disulfiram
* aversive conditioning for alcoholics * causes acute physical distress from alcohol use
135
Naltrexone
* opioid receptor antagonist * **reduces rewarding effects of drug use** * for **opioid addicts and alcoholics**
136
Acamprostate
* NMDA receptor antagonism * **reduces reinforcing effects** of drug * for **alcohol**
137
Amphetamine/Methamphetamine
* **evoke release of catecholamines** in periphery and CNS * _symptoms_: **↑ HR, ↑ or ↓ BP, ↑RR, hyperthermia, mydriasis, euphoria, ↑ speech**. * _overdose_: **anxiety, agitation, paranoia, seizures, arrhytmias, MI, cerebral hemorrhage, rhabdomyolysis**
138
Cocaine/Methylphenidate
* CNS effects from **blocked DA reuptake** * _sympthoms_: **↑ HR, ↑ or ↓ BP, ↑ RR, hyperthermia, mydriasis, euphoria, ↑ speech** * _overdose_: **anxiety, agitation, paranoia, seizures, arrhythmias, MI, cerebral hemorrhage, rhabdomyolysis**
139
MDMA/Ecstasy
* **release 5-HT ** * have **mild hallucinogenic effects** * similar to amphetamines
140
LSD/Mescaline
* **5-HT2A partial agonist** * symptoms: **↑HR, ↑or↓ BP, ↑RR, mydriasis, nausea, altered perceptions with panic/anxiety** * OD not life threatening
141
Phencyclidine/Ketamine
* **NMDA receptor antagonist** * _symptoms_: **euphoria, hallucinations, agiation/violent behavior, psychosis, catatonia, anxiety/panic, ↑HR, ↑BP, ↑RR, miosis, nystagmus, rhabdomyolysis** * _overdose_: go to coma, seizures, renal failure, death
142
Cannabinoids
* THC * use: anorexia from AIDs, prevent nausea/vomiting during chemo * _symtpoms_: **euphoria, conjunctivitis, ptosis, ↑HR, appetite**
143
Anandamide
* aka AEA * endocannabinoid * activates CB2 and CB1 receptors * released from Ca influx that N-acyl transferase
144
2-AG
* endocannabinoid * activates CB1 and CB2 receptors * released with Ca influx activating phospholipase C
145
Rimonobant
* CB1 antagonist * use: obesity (↓ appetite) * side effects: depression, off the market
146
Nicotine Withdrawal
* irritability, impatience, hostility * anxiety * depressed mood * difficulty concentrating * restless * ↓ HR * ↑ appetite or weight gain
147
Acute Opioid Withdrawal
* peaks in 36-72hr * **drive for drug** * begins 8-12 hr, peaks in 48-72 hr * tearing, runny nose, yawning, **sweating** * begins 12-14hr, peaks in 48-72hr * ​restless sleep * begins in 12hr, peaks 48-72 hr * **dilated pupils, anorexia, goosebumps**, irritability, tremor * at peak * **insomnia**, violent **yawning**, weakness, GI upset, **chills, flushing**, muscle spasm, ejaculation, abd pain
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Blood Ethanol Concentration 15-50 50-100 100-200 200-300 300-400 \>500
* 15-50 = 0.015-0.05: * modest impairment to drive * 50-100 = 0.05-0.1: * impaired motor function, sedation, euphoria * 100-200 = 0.1-0.2: * emotional instability, slurred speech, ataxia, analgesia * 200-300 = 0.2-0.3: * emesis, stupor * 300-400 = 0.3-0.4 * coma * \>500 = \>0.5 * respiratory depression, death
149
Moderate Alcohol Dose High Dose
* moderate = cutaneous vasodilation, ↑ HDL levels, ↓ risk atherosclerosis and CV mortality * high = toxic effects, ↓ CO and muscle strength. contributes to cardiomyopathy, muscle weakness, nutritional deficiencies.
150
Alcohol and GI Fnct
* \>40% irritates gastric mucosa * cause inflammation, erosive gastritis with chronicity * potentiates ulcerogenic effects of other drugs
151
Alcohol and Liver
* causes ↑ acetyl-CoA, ↓ NAD+ * leads to fatty liver, alcoholic hepatitis, cirrhosis
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Alcohol and Kidney
* inhibits ADH release, ↑ output of dilute urine
153
Alcohol and Sexual Fnct
* ↑ desire but ↓ physio response and performance
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Cytosolic Alcohol Dehydrogenase
* converts ethanol to acetaldehyde * rate limiting step for ethanol, methanol, ethylene glycol * zero order kinetics * plateaus at 7-10g/hr (1 drink per hour)
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Microsomal Ethanol Oxidixing System (MEOS)
* hepatic P450 enzyme * chronic alcohol use causes drug interactions
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Mitochondrial Acetaldehyde Dehydrogenase
* converts acetaldehyde to acetate
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Ethanol Clinical Uses
* nerve lysis for intractable pain * methanol or ethylene glycol poisoning
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Chronic Alcoholism
* tolerance * cross-tolerance with benzo, barbiturates, sedatives * physical and psychological dependence * can have: **peripheral neuropathy** (weakness, tingling, numbness) or **Wernike encephalopathy, liver toxicity, GI toxicity** * _withdrawal_: severe = **delirium tremens - tremor, delirium, hallucinations, fever, autonomic instability, seizures**
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Wernike Encephalopathy
* aka wet brain * **oculomotor paralysis, ataxia, confusion** * **go to coma and death** * from **thiamine** deficiency * goes to **_Korsakoff's psychosis_** = irreversible memory impairment and loss of contact with reality
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Fetal Alcohol Syndrome
* from chronic alcohol abuse during pregnancy * causes: **narrow forehead** * **short paplebral fissures,** * **small nose,** * **small midface,** * **long upper lip with deficient philtrum,** * **microcephaly** * **attentional and intellectual deficits,** * **mental retardation.**
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17beta-estradiol
* most important physio **estrogen** * has **aromatic** as part of ring * eliminated by liver, poor oral availability * transdermal patches avoid 1st pass * _use_: **post menopausal therapy**
162
Estrogen
* works through **E2 to stimulate growth and induces P receptors.** * important for female reproductive tract and breast * with P, helps regulate LH and FSH * **E2 ⇒ ↓LDL, ↑HDL, ↑ triglycerides** * _premenopause side effects_: altered skin pigmentation, ↑ risk gallbladder disease, nausea, breast tenderness, headache, ↑ risk VTE, ↑ risk MI and stroke, ↑ risk uterine cancer * _post menopause additional side effects_: ↑ risk breast cancer
163
Progestin
* works thru **P to direct functional differentiation during luteal phase and pregnancy** * prevents development of uterine cancer from unopposed estrogen * side effect: acne, ↑ body hair, weight gain, ↑ risk infertility, ↑ risk breast cancer
164
Estrone Sulfate
* **conjugated estrogen** * **absorbed in lower GI tract** * forms estrone after enzymatic hydrolysis * _use_: oral **hormone replacement in post-menopausal women**
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Equiline Sulfate
* **conjugated estrogen** * **absorbed in lower GI tract** * forms equiline from enzymatic hydrolysis * _use_: oral **hormone replacement in post-menopausal women**
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Estradiol Valerate
* **esterified estrogen** * parenteral injection in oil * slowly released, **prolonged delivery of 17beta-estradiol (2-4wks)** * **↓ hepatic effects of estrogens** * use: hypogonadism
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Estradiol Cypionate
* **esterified estrogen** * parenteral injection * slowly released, **prolonged delivery 17beta-estradiol (2-4wks)** * **↓ hepatic effects estrogen** * use: **hypogonadism**
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Ethinyl Estradiol
* **synthetic steroidal estrogen** * 17-ethinyl substitution ⇒ **↓ 1st pass effect** * t1/2= 13-27hr * _use_: **combo oral contraceptives, hypogonadism**
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Mestranol
* **synthetic steroidal estrogen** * 17-ethinyl substitution ⇒ **↓ 1st pass effect** * t1/2 = 13-27hr * _use_: **combo oral contraceptives**
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Diethylstilbesterol (DES)
* **synthetic non-steroidal estrogen** * potent, prolonged effects * relieves bone pain, improves quality of life * _use_: **palliative tx of advanced prostate or breast cancer** * _side effect_: cardiovascular toxicity (**thromboembolism, stroke, fluid retention**)
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Medroxyprogesterone Acetate
* **21-carbon analog of progesterone** * in DepoProvera * **anti-aldosterone** effects, **inhibits LH and FSH release** * _use_: **hormone replacement in post-menopausal women**
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Megestrol Acetate
* **21-carbon analog of progesterone** * has **anti-aldosterone effects** * **inhibits LH and FSH release** * _use_: **stimulate appetite and weight gain in AIDS pts**
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Norethindrone
* **19-norestosterone derivative** * has 17-ethinyl group, good bioavailability * makes decidual change in endometrium * **weak androgen and antiestrogen effects** * strong **inhibitor of LH and FSH release** * _use_: **combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive**
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Levonorgestrel
* **19-norestosterone derivative** * has 17-ethinyl group, good bioavailability * makes **decidual change in endometrium** * **weak androgen and antiestrogen effects** * strong **inhibitor of LH and FSH release** * _use_: **combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive**
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Norethynodrel
* **19-norestosterone derivative** * has 17-ethinyl group, good bioavailability * makes decidual **change in endometrium** * **estrogenic effects** * **strong inhibitor of LH and FSH release** * _use_: **combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive**
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Desogestrel
* **19-norestosterone derivative** * has 17-ethinyl group, good bioavailability * makes decidual change in endometrium * minimal androgenic or estrogenic effects * strong **inhibitor of LH and FSH release** * _use_: **combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive**
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Norgestimate
* **19-norestosterone derivative** * has 17-ethinyl group, good bioavailability * makes decidual change in endometrium * **minimal androgenic or estrogenic effects** * **strong inhibitor of LH and FSH release** * _use_: **combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive**
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Dienogest
* **19-norestosterone derivative** * has 17-ethinyl group, good bioavailability * makes decidual change in endometrium * **antiandrogenic ** * strong **inhibitor of LH and FSH release** * use: **combo oral contraceptive, progestin mini-pill, contraceptive patch, emergency post-coital contraceptive**
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Ulipristal Acetate
* **selective progesterone receptor modulator (SPRM)** * agonist and antagonist effects * prevents ovulation and impairs implantation * **60% effective when started within 120hr of intercourse** * _use_: **emergency contraception** * _side effect_: **headache, nausea, dysmennorhea**
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Testosterone
* poor bioavailability * rapid hepatic metabolism * T gels and patches for slow transdermal delivery
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Testosterone Ethanate
* **parenteral esterified testosterone** * converted to testosterone * no hepatotoxicity * inject every 2-4wks * _use_: **induce purbertal changes in hypogonadal boys**
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Testosterone Cypionate
* **parenteral esterified testosterone** * converted to testosterone * inject every 2-4wks * _use_: **induce pubertal changes in hypogonadal boys**
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Methyl Testosterone
* **orally active androgen**, anabolic steroid * has 17-alkyl substitution * **dose related hepatotoxicity**
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Fluoxymesterone
* **orally active androgen**, anabolic steroid * has 17-alkyl substitution * **dose related hepatotoxicity**
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Oxandrolone
* **orally active androgen**, anabolic steroid * has 17-alkyl substitution * **dose related hepatotoxicity**
186
Danazol
* **synthetic steroid derivative ** * 17-ethinyl group * mix of weak androgen, antiestrogen, progestin, glucocorticoid activity * **inhibits ovarian function, ↓ LH and FSH** * _use_: **endometriosis, prevent episodes of hereditary angioneurotic edema in pts with complement C1 inhibitor deficiency**
187
Combo Oral Contraceptive
* mix of estrogen and 19-nortesterosterone/progestin analog * estrogen inhibits ovulation and ↓ fertility * progestin enhances estrogen actions and provides normal cycling with estrogen withdrawal * _use_: **dysmenorrhea, acne, hirsutism**
188
Monphasic Combination Contraceptive
* fixed dose estrogen and progestin * 99-100% effective * _use_: **dysmenorrhea, acne, hirsutism**
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Biphasic or Triphasic Combo Contraceptive
* varied dose progestin and/or estrogen * reduces spotting * _use_: **dysmenorrhea, acne, hirsutism**
190
Progestin Only Contraceptive
* daily mini pills of progestin (19-nortestosterone derivative) * _use_: when estrogen contraindicated, **dysmenorrhea, endometriosis** * _side effect_: **weight gain, abnormal bleeding, delayed onset fertility, ↑ risk osteoporosis**
191
Plan B = Levonorgestrel
* 2-4 oral combo contraceptive pills or progestin alone contraceptive pills * 80% effective when begun within 72hrs * _use_: **emergency contraception** * _side effect_: **nausea**
192
Preven = Levonorgestrel + EE
* 2-4 oral combo contraceptive pills or progestin alone pills. * **80% effective when started within 72 hr** * _use_: **emergency contraceptive** * _side effect_: **nausea**
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Flutamide
* **androgen receptor (AR) antagonist, non-steroidal** * markedly **↑ plasma testosterone levels** * _use_: **prostate cancer therapy with GnRH super-agonist**, prevent flare-up of tumor * _side effect_: **gynecomastia**
194
Bicalutamide
* **potent non-steroidal androgen receptor antagonist** * markedly **↑ plasma testosterone levels** * less hepatotoxic than flutamide * _use_: **prostate cancer therapy with GnRH super-agonist**, prevent tumor flare * _side effect_: **gynecomastia**
195
Spironolactone
* weaker **androgen receptor antagonist** * _use_: **hirsutism** * _side effect_: **gynecomastia**
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Finasteride
* **5alpha-reductase inhibitor**, prevents dihydrotestosterone synthesis * _use_: **benign prostatic hypertrophy**, male pattern baldness * _side effect_: **2% sexual dysfunction**
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Dihydrotestosterone (DHT)
* androgen derivative
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Tamoxifen
* **non-steroidal estrogen receptor antagonist** * aka selective estrogen receptor modulators * **estrogen antagonist on breast** * **estrogen agonist on bone** * **partial estrogen agonist on uterus** * _use_: **ER-pos breast cancer**, prevention of breast cancer in high risk, tx/prevention of **osteoporosis, infertility** * _side effect_: **↑ risk uterine cancer, ↑ risk VTE**
199
Clomiphene
* **non-steroidal receptor antagonist** * aka selective estrogen receptor modulator (SERM) * **leads to loss of estrogen feedback inhibition** on hypothalamic pituitary axis ⇒ ↑ LH and FSH * _use_: **infertility in women with impaired release of LH and FSH** * _side effect_: **↑ risk VTE**
200
Raloxifene
* **non-steroidal estrogen receptor antagonist** * aka selective estrogen receptor modulator (SERM) * estrogen **antagonist on breast** * not as strong as tamoxifen * estrogen **agonist on bone** * _use_: tx/prevention **breast cancer, osteoporosis, infertility** * _side effect_: **↑risk VTE, risk uterine cancer**
201
Anastrazole
* **aromatase inhibitor** (CYP19), **non-steroidal** * don't convert androgen to estrogen * _use_: **breast cancer resistant to tamoxifen** * _side effect_: ↑ risk **osteoporosis**
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Fluvestrant
* **steroidal anti-estrogen** = estrogen receptor antagonist * **impairs estrogen receptor dimerization and retention in nucleus, promote receptor degradation**. * _use_: **advanced breast cancer resistant to therapy** * _side effect_: ↑ risk **osteoporosis**
203
Mifepristone
* **progesterone receptor antagonist** * **blocks glucocorticoid receptors** * use during 1st 7 wks conception * **95% effective** in terminating pregnancy * use with misprostol to promote expulsion of aborted fetus * _use_: **1st trimester abortion** * _side effect_: **nausea, vomiting, diarrhea, vaginal bleeding**
204
Drospirenone
* **anti-mineralcorticoid** * no androgenic activity * **less bloating and breast tenderness than 1-nortesterone related progestins**
205
Androgen
* such as testosterone * stimulates spermatogenesis * _use_: **↑ sperm counts in infertile men, hypogonadism, endometriosis, hereditary angioneurotic edema, cancer therapy** * _side effects_: ↑ muscle mass, linear growth, virilizing effects (sex organs, body hair, larynx), closure of epiphyses of long bones, **hepatotoxicity, jaundice, acne, ↑ aggression**
206
Exemestane
* **non-steroidal aromatase inhibitor** (CYP19) * don't convert androgens to estrogens * _use_: **breast cancer resistant to tamoxifen** * _side effect_: **↑ risk VTE**

Pharmacology (6 decks)

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