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1.9
PHAR 422 & 423
Drug | Use | Event |
---|---|---|
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 |