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1.9

PHAR 422 & 423

DrugUseEvent
Famotidine (Pepcid) H2 Antagonist; Acid relief Thrombocytopenia
Esomeprazole (Nexium) PPI; Decreased acid secretion Does not cause burping
Magnesium hydroxide (Milk of Magnesia) Osmotic laxative; Constipation Diarrhea
Omeprazole (Prilosec) PPI; Decreased acid secretion Cannot be used safely with Plavix
Ranitidine (Zantac) H2 Antagonist; Acid relief Second longest antacid secretion effect
Aluminum salts (Sucralfate) Mucosal protectant; Neutralizes acid Constipation
Promethazine (Phenergan) D2 antagonist, M1 antagonist, H1 antagonist; Nausea and vomiting Movement disorder
Erythromycin (EES) Gastroparesis (not constipation) QTc prolongation
Alosetron (Lotronex) 5-HT3 antagonist; IBS-D in women Not used for nausea
Gastrin increases Calcium, which increases Stomach acid secretion
Acetylcholine increases Calcium, which increases Stomach acid secretion
Prostaglandin E1 decreases cAMP, which decreases Stomach acid secretion
Norepinephrine No effect on cAMP or calcium No effect on stomach acid secretion
Histamine decreases cAMP, which decreases Stomach acid secretion
Myenteric plexus is also known as Auerbach's plexus, and controls GI tract motility
Meissner's plexus is also known as Submucous plexus, and controls Mucosal activities and GI blood flow
What do prostaglandins do in the stomach? Stimulates mucous and HCO3 secretion, inhibits acid secretion as well; What do prostaglandins do in the pancreas Similar process in pancreas
Mouth Produces enzymes for digesting proteins
Esophagus Conduit with peristalsis but no segmentation contractions
Stomach Produces enzymes for digesting proteins
Small intestine Absorption of the MOST water
Large intestine Mass movement but no migrating motor complex
Pancreas Secretes bicarbonate into small intestine, releases collagenase into gut
Urea in a patient's breath indicates what? H. pylori
Metoclopramide (Reglan) D2 antagonist; Nausea and vomiting
Bisacodyl Stimulant laxative; Constipation
Linaclotide (Linzess) IBS-C
Erythromycin (EES) Gastroparesis
Diphenoxylate/Atropine (Lomotil) Mu agonist; Antidiarrheal
Lubiprostone (Amitiza) ClC-2; Constipation
Senna (Senokot) Stimulant laxative
Somatostatin decreases enzyme release in the Pancreas
Norepinephrine increases motility in the Gut
True/False: Amylin reduces post-prandial glucose intake. True
True/False: Histamine increases stomach acid secretion. True
True/False: GLP-1 increases insulin release. True
True/False: CDAD is an adverse effect of PPIs True
True/False: Impaired vitamin B12 absorption is an adverse effect of PPIs True
True/False: A stimulant laxative would be best for a movement disorder. True
What drug induces uterine contraction? Misoprostol (PGE1 analogue)
What drug darkens the tongue and stools? Bismuth subsalicylate
What drug is used for the healing of a fistula? Octreotide
What is the longest acting 5HT-3 antagonist? Palonosetron (Aloxi)
True/False: H. pylori can be treated but requires a PPI or bismuth compounds. True
True/False: Drugs that block the post-synaptic D2 receptor are antipsychotics or for nausea and vomiting. True
Docusate (Colace) Stool Surfactant
True/False: Bloody diarrhea should not be treated with antidiarrheals. True
Loperamide (Imodium) Mu agonist; Antidiarrheal
What must the proximal urinary sphincter do for storage? Contract; Why? It's an internal urinary sphincter
What must the proximal urinary sphincter do for voiding? Relax; Why? It's an internal urinary sphincter
What must the distal urinary sphincter do for storage? Contract; Why? It's an external urinary sphincter
What must the distal urinary sphincter do for voiding? Relax; Why? It's an external urinary sphincter
What must the detrusor muscle do for storage? Relax; Why? It's responsible for expulsion of urine
What must the detrusor muscle do for voiding? Contract; Why? It's responsible for expulsion of urine
What does an M3 antagonist at the salivary gland do? Dry mouth; What does an M3 agonist at salivary gland do? Salivation
What does an M3 antagonist at the airways do? Bronchodilation; What does an M3 agonist at the airways do? Bronchoconstriction
What does an M3 antagonist at the CNS for mental status do? Decreases memory and cognition; What does an M3 agonist at the CNS for mental status do? Normal mentality?
What does an M2 antagonist at the heart do? Tachycardia and palpitations; What does an M2 agonist at the heart do? Bradycardia?
What does an M3 antagonist at the gut do? Constipation, decrease acid secretion; What does an M3 agonist at the gut do? Diarrhea, acid secretion
What does an M3 antagonist in the bladder do? Causes less urges to void; What does an M3 agonist in the bladder do? More voidance?
Which M3 antagonists work best for urinary incontinence? Oxybutynin (Ditropan + XL), Tolterodine (Detrol + LA), Trospium (Sanctura), Darifenacin (Enablex), Solifenacin (Vesicare), Fesoterodine (Toviaz)
What beta-3 agonist works best for urinary incontinence? Mirabegron (Myrbetriq)
What is Zollinger-Ellison Syndrome? Gastrin-secreting tumor. What drugs are used to treat it? PPIs
A patient with GERD complains of symptoms at night and takes his medication in the morning. What would you recommend? Add Famotidine or antacids at bedtime
Would changing Oxybutynin (Ditropan + XL) to Tolterodine (Detrol + LA) help with confusion? Yes, it is a prodrug and has less CNS penetration
Would changing Oxybutynin (Ditropan + XL) to Darifenacin (Enablex) help with confusion? Yes, there is less CNS penetration than Oxybutynin (Ditropan + XL) and Darifenacin (Enablex)
Would changing Oxybutynin (Ditropan + XL) to Mirabegron (Myrbetriq) help with confusion? Yes, it targets B3 receptors, not muscarinics
Would changing Oxybutynin (Ditropan + XL) to Toviaz (Fesoterodine) help with confusion? Yes, it's a prodrug with the same active ingredient as Tolterodine (Detrol + LA)
Would Mirabegron (Myrbetriq) or Solifenacin (Vesicare) be better for someone with hypertension? Solifenacin (Vesicare); Why? Mirabegron (Myrbetriq) has HTN adverse effect, and Solifenacin (Vesicare) has better selectivity for bladder M3 receptors.
How does tumescence (volume expansion) of penile tissue occur? Rapid vasodilation, inhibition of venous drainage Parasympathetic nervous system in play
How does the release of nitric oxide of the endothelial cells results in erection? Nitric oxide is a vasodilator. It triggers the enzyme guanylate cyclase to convert GTP to cGMP, which leads to decrease in calcium. Decreased calcium results in smooth muscle relaxation (vasodilation)
What is priapism? Painful erection that lasts more than 6 hours. Can cause prolonged hypoxia (low oxygen) which can result in permanent tissue damage
Red Ginseng (Korean Panax use? Erectile dysfunction
Is it okay to take Tadalafil (Adcirca, Cialis) and Ritonavir the same time? No. Ritonavir is a strong CYP3A4 inhibitor and it cannot be taken the same time as Tadalafil (Adcirca, Cialis) a PDE5 inhibitor. PDE5 effect is reduced.
Is there an alternative to taking Taladafil (Adcirca, Cialis) and Ritonavir together? Yes, Alprostadil (MUSE, Caverjet, Edex) is a PGE1 used in patients who can't use PDE5
Who can benefit from testosterone for erectile dysfunction and how should the medication be used? Patients with low testosterone levels; Testosterone must be used daily for effective treatment of erectile dysfunction.
How is oral nitrate dangerous with a PDE5 inhibitor? It causes hypotension.
Is Alprostadil MUSE effective for erectile dysfunction? Yes
Is Amitriptyline effective for erectile dysfunction? No, it causes erectile dysfunction.
Is Apomorphine (Apokyn) effective for erectile dysfunction? Questionable effectiveness
Is Diphenhydramine effective for erectile dysfunction? No, it causes erectile dysfunction.
Is Yohimbine (alpha-2 antagonist) effective for erectile dysfunction? Yes
Is Solifenacin (Vesicare) effective for erectile dysfunction? No, used for urinary incontinence
Is Phentolamine-papaverine (alpha antagonist) effective for erectile dysfunction? Yes, it decreases vasoconstriction
How do hormones differ from drugs? Higher TI, endogenous control mechanisms, one hormone has effects in many unrelated organs
Humoral hormones Changing levels of ions in blood triggers hormone release
Neural hormones Nerves stimulate hormones
Hormonal hormones Hormones stimulate other hormones release
What are four general roles of hormones in therapy? Replacement therapy, decrease endogenous hormone synthesis, diagnose endocrine pathophysiology, non-endocrine diseases
What hormones are synthesized/released by the anterior pituitary gland? TSH, ACTH, FSH, LH, GH, PRL, MSH
What is the function of tropic hormones (TSH, ACTH, FSH, LH) Regulate functions of other hormones/glands
What hormones are synthesized/released by the posterior pituitary gland? ADH, Oxytocin
What is the function of Oxytocin? Smooth muscle contraction in reproductive tracts, labor and lactation in females
What is the function of ADH (antidiuretic hormone [vasopressin])? Tells kidney to retain water from urine, increases blood pressure
How is the hypothalamus feedback inhibited? Hypothalamus --H1--> Anterior pituitary --H2--> Endocrine gland --H3--> Tissue; H2 inhibits hypothalamus, and H3 inhibits hypothalamus and anterior pituitary
How does Cortisol cause negative feedback? It is released from adrenal cortex (H3) and blocks H1 and H2 from hypothalamus and anterior pituitary, respectively.
Explain the levels of integration in endocrine and how it is used in diagnoses of endocrine function using CRH-ACTH-Cortisol loop? If CRH is high, everything else is too. If CRH is low but ACTH is high, then the Cortisol will be high. If only Cortisol is high, then nothing else will be effected.
What are some positive feedback mechanisms for GH? GHRH and ghrelin, vigorous exercise, stress, insulin-induced hypoglycemia, arginine.
What are two negative feedback mechanisms for GH? SST (Somatostatin), IGF-1
What are the effects of GH on the body? Anabolic and lipolytic (and diabetogenic) effects, growth of every organ and tissue except brain and eye, direct and indirect effects
What are two indications for GH replacements in children and adults? Short stature associated with Turner or Noonan Syndrome in children, GH deficiency, AIDS-related wasting in adults
What is Somatropin? GH analogue
What is the drawback of Somatropin? IM or SQ injection and slow absorption
How is Somatropin's response monitored? Every 3 to 4 months by X-ray
What are ADR of Somatropins? Pre-existing tumors progress in peds (rare), hypothyroidism, type II diabetes, scoliosis, intracranial hypertension (vision, HA, N/V), antibodies development, arthralgias, myalgias, carpal tunnel, musculoskeletal pain, fluid retention.
What is Mecasermin (Increlex) and its indication? IGF-1 used in children with growth failure that does not respond to exogenous GH
List three ADRs of Mecasermin (Increlex) Intracranial hypertension, high liver function tests, hypoglycemic potential
What are two conditions of GH excess? Gigantism and acromegaly
How do you treat GH excess? Somatostatin (SST) and Somatostatin analogue (Octreotide, Lanreotide); what are their MOAs? Somatostatin (SST) ---> inhibits GH, TSH, PRL, insulin, glucagon, and GI hormones; Somatostatin analogues (Octreotide, Lanreotide) ---> SST agonist
What are ADRs of Somatostatin analogues (Octreotide, Lanreotide)? 25% gallstones, 50% GI effects, hyperglycemia (rare), injection site reactions
What is prolactin and state its functions? Pituitary hormone ---> binds breasts and other tissues, induces growth and differentiation of ductal and luboalveolar epithelium; causes lactation and milk
What cells synthesize prolactin? Lactotropes
How is prolactin regulated? Prolactin release inhibiting hormone (PRIH) is dopamine
What drugs affect prolactin levels? Dopamine antagonists ---> Haloperidol and Chlorpromazine
How do you treat hyperprolactinemia? Bromocriptine (Parlodel), Cabergoline (Dostinex)
List three gonadotropins? LH, FSH, hCG
Where is the site of action of LH? Leydig cells (males), corpus luteum and thecal cells (females)
Where is the site of action of FSH? Sertoli cells (males), Granulosa cells (females)
Where is the site of action hCG? From placenta ---> maintains corpus luteum after LH
How does botulism prevent muscle contraction? It inhibits the release of acetylcholine which prevents muscle contraction.
Which spasmolytics have dry mouth effects? Orphenadrine (Norflex) and Tizanidine (Zanaflex)
What is Baclofen (Lioresal)? Oral spasmolytic most established to exert effects at the spinal cord.
What neuromuscular blocker can have its effects reversed by nicotine? Vecuronium (Norcuron)
What properties does Succinylcholine (Anectine) possess? Muscle paralysis effect, hyperkalemia ADR
What spasmolytic is best for malignant hyperthermia or neuroleptic malignant syndrome? Dantrolene
What are two possible side effects for Cisatracurium (Nimbex)? Bronchoconstriction and risk of anaphylaxis
What are some side effects of Succinylcholine (Anectine) Bradycardia, hyperkalemia, excessive salivation, cardiac arrhythmia, further damage to bone in bone-fractured patients
MOA for Succinylcholine (Anectine) Nicotinic agonist
MOA for Tizanidine (Zanaflex) Alpha-2 adrenergic agonist
MOA for Metaxalone (Skelaxin) Unknown, but in CNS
MOA for Norflex (Orphenadrine) H1 antagonist
MOA for Valium (Diazepam) Enhance GABA binding to GABA-A receptor
MOA for Baclofen (Lioresal) GABA-B agonist
Sedation is caused by All spasmolytics
Cimetidine (Tegamet) H2 Antagonist; Acid relief Hyperprolactinemia, also may reduce patient's testosterone effects
Created by: sdeck86
 

 



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