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Cholinergics

Cholinergics. Sara Trovinger PharmD. Indications 1. Cause SLUD: salivation, lacrimation, urination, and defication Used for contaction of muscles, bronchoconstriction, bradycardia Frequently used in eye drops to cause contraction of the iris

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Cholinergics

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  1. Cholinergics Sara Trovinger PharmD

  2. Indications1 • Cause SLUD: salivation, lacrimation, urination, and defication • Used for contaction of muscles, bronchoconstriction, bradycardia • Frequently used in eye drops to cause contraction of the iris • Examples: Acetylcholine, Bethanechol, Pilocarpine, Carbachol

  3. Contraindications2 • Asthma • GI spasm • Acute heart failure • Hyperthyroidism • Parkinson’s disease • Peptic ulcer disease • Urinary tract obstruction

  4. Possible Adverse Effects2 • Cardiovascular: Bradycardia, flushing, hypotension • Ocular: Clouding, corneal edema • Respiratory: Dyspnea • Diaphoresis

  5. Sedatives

  6. Indications3 • Relief of anxiety • Insomnia • Sedation and amnesia before and during medical procedures • Treatment of epilepsy and seizure states • Control of withdrawal states • Muscle relaxation in specific neuromuscular disorders

  7. How They Work3 • Bind to GABAA receptor • GABA is a major inhibitory neurotransmitter • Benzodiazepines potentiate the effect of GABA inhibition, increasing the frequency of chloride ion channel opening • Barbituates appear to increase the duration that these channels are open

  8. Examples3 • Benzodiazepines • Diazepam • Lorazepam • Midazolam • Barbiturates • Pentobarbital • Phenobarbital • Miscellaneous • Chloral hydrate • Hydroxyzine

  9. Contraindications3 • Increased sensitivity seen in patients with: • Cardiovascular disease • Respiratory disease • Hepatic impairment • COPD • Sleep apnea • Elderly • Barbiturates contraindicated: • Acute intermittent porphyria • Variegate porphyria • Hereditary coproporphyria • Systemic porphyria

  10. Adverse Events3 • Drowsiness • Impaired judgment • Diminished motor skills • Respiratory Depression • Dependence • Withdrawal

  11. References • Drug Classes : Cholenergics. Access Pharmacy [database online]. Available at: http://accesspharmacy.mhmedical.com/drugs.aspx. Accessed August 27, 2014. • Drug Monographs: Acetylcholine. Access Pharmacy [database online]. Available at: http://accesspharmacy.mhmedical.com/drugs.aspx?GbosID=130728. Accessed September 4, 2014. • Trevor, Anthony and Walter Way. Basic and Clinical Pharmacology. McGraw-Hill Companies Inc. 2012. Web.

  12. Anticholinergics Trenton Shoda PharmD Candidate Purdue University

  13. Indications • Relieve cramps/painful menstruation or spasms of the stomach, intestines, and bladder • In combination w/antacids for treatment of peptic ulcers • Prevent nausea, vomiting, and motion sickness • Surgery and emergency procedures • Runny nose • Asthma • Diarrhea • Excessive saliva production

  14. How do they work? • Anticholinergic agents block acetylcholine's action by competitively binding and blocking muscarinic receptors.

  15. Contraindications • Elderly • Dementia • Gastrointestinal obstruction • Glaucoma • Ulcerative Colitis • Breastfeeding

  16. Possible Side Effects

  17. Antiemetics

  18. How do they work? • Antihistamines – block H1 receptors centrally and in middle ear • Anticholinergics - blockage of central muscarinic receptors • Benzodiazepines – inhibitory effect on vomiting center and general CNS depression • Corticosteroids – inhibition of prostaglandin activity • Serotonin Antagonists – selective 5-HT3 receptor antagonist peripherally on vagal nerve terminals and centrally in the chemoreceptor trigger zone

  19. Contraindications • Hypersensitivity • Narrow angle glaucoma – Benzodiazepines • Corticosteroids • Glaucoma • Current infection

  20. Possible Side Effects • Decrease in appetite • Constipation • Fatigue • Reduced Libido • Lightheadedness • Hypertension

  21. Narcotics/Analgesics

  22. How do they work? • NSAIDs & Acetaminophen – inhibition of prostaglandin synthesis • Opioids – react with opioid mu-receptors in the central nervous system

  23. Contraindications • NSAIDs • Hypersensivity • <18 yo (aspirin) • Acetaminophen • Active and severe hepatic disease • Hepatic impairment • Hypersensitivity • Opioids • Respiratory depression • Hypersensitivity • Hypercarbia

  24. Possible Side Effects • Hypotension • Constipation, Nausea, Vomiting • Dizziness, Lightheadedness, Sedation • Increased risk of bleeding

  25. References • Norco.  DrugPoints Summary.  Micromedex 2.0.  Truven Health Analytics, Inc. Greenwood Village, CO.  Available at: http://www.micromedexsolutions.com.  Accessed September 5, 2014.

  26. Laxatives Claire McClain 2015 PharmD Candidate Purdue College of Pharmacy

  27. Indications • Encourage bowel movements to relieve constipation • Bowel evacuation before gastrointestinal procedures

  28. How do they work? • Bulk laxatives: stimulate peristalsis by causing the retention of fluid and an increase in mass of fecal material (psyllium, polycarbophil) • Stimulant laxatives: increase muscle contractions to move the stool along by directly stimulating nerve endings (bisacodyl, senna) • Osmotic laxatives: draw water into the intestine from surrounding tissues resulting in a bulky soft stool to stimulate peristalsis ( saline laxatives, Lactulose, sorbitol) • Stool softeners: help to mix liquids in the stool and prevent hard, dry stools(docusate) • Lubricant laxatives: coat the stool and intestinal track to keep water in the stool (mineral oil)

  29. Contraindications • Patients with signs of appendicitis or inflamed bowel • Not intended for patients who miss only a day or two of bowel movements • Patients with a documented allergic reaction to any of these medications • Children under 6 years of age unless prescribed by a doctor • Avoid saline laxatives in patients with reduced kidney function

  30. Possible adverse effects • Increased blood sugar in diabetic patients • Exacerbation of heart disease or high blood pressure • Mineral oil can increase a patient’s risk of pneumonia • Diarrhea, bloating, cramping, belching • Difficulty swallowing (lump in throat) • Overuse of some laxatives has caused damage to the nerves, muscles, and tissues of the intestines and bowel. 

  31. Corticosteroids

  32. Indications • Anti-inflammatory agent • Immunosuppressant • Used in active ulcerative colitis and Crohn's disease

  33. How do they work? • Closely resemble cortisol, a hormone produced by the adrenal glands • Reduce the production of inflammatory chemicals • Reduce the activity of the immune system by altering the function of white blood cells • Induce remission in patients with inflammatory bowel disease • Examples include: prednisone, prednisolone, methylprednisolone, belcometasone

  34. Contraindications • Acute infections uncontrolled by antimicrobial therapy • Patients with active tuberculosis • Caution in patients with heart failure, recent myocardial infarction, diabetes, or hypertension • Caution in septic shock patients

  35. Possible Adverse Effects • Mood swings, irritability • Weight gain, increased appetite • Increased risk of infection • Puffy face, water retention • Increased blood sugar • Increased blood pressure • Easy bruising • Slower wound healing • Osteoporosis (long term)

  36. Possible Adverse Effects • CUSHINGOID • C – CataractsU – UlcersS – Striae, Skin thinningH – Hypertension, HirsutismI – Immunosuppression, InfectionsN – Necrosis of femoral headsG – Glucose elevationO – Osteoporosis, ObesityI – Impaired wound healingD – Depression/mood changes

  37. Sclerosants5

  38. Indication • Acute endoscopic hemostasis • Elective obliteration of bleeding esophageal varices • Can be used alone or in combo with ligation for the treatment of bleeding esophageal or junctionalvarices • Not indicated for primary prophylactic treatments of varices that have not bled

  39. How do they work? • Tissue irritants that cause vascular thrombosis and endothelial damage • Leads to endofibrosis and vascular obliteration when injected into adjacent blood vessels • Most are fatty-acid derivatives (sodium morrhuate, ethanolamine oleate) ,synthetic chemicals (sodium tetradecyl sulfate, polidocanol), or alcohols (ethanol) • Dispensed with a sclerotherapy needle passed through the working channel of an endoscope

  40. Possible adverse effects • Chest pain • Mucosal ulceration • Bleeding • Esophageal strictures and fistulas • Pleural effusions • Sepsis/bactermia • Pneumonia • Hypoxia * Complications may occur in as many as 25% of patients

  41. Contraindications • Patients with cirrhosis and patients who are immunocompromised are at a greater risk for bacteremia • Caution in patients with: • Mechanical prosthetic devices • History of endocarditis • Vascular grafts • Surgical systemic-pulmonary shunts • Ascites

  42. References • Laxatives. DrugPoints Summary. Micromedex 2.0. Truven Health Analytics, Inc. Greenwood Village, CO. Available at: http://www.micromedexsolutions.com. Accessed August 27, 2014. • Cleavland Clinic. Drugs and Supplements. Available at: http://my.clevelandclinic.org/drugs/corticosteroids/hic_corticosteroids.aspx. Accessed August 27,2014. • Mayo Clinic. Prednisone and other corticosteroids. Available at: http://www.mayoclinic.org/steroids/art-20045692?pg=2. Accessed August 27,2014. • Corticosteroids.DrugPoints Summary. Micromedex 2.0. Truven Health Analytics, Inc. Greenwood Village, CO. Available at: http://www.micromedexsolutions.com. Accessed August 27, 2014. • Croffie J, Somogyi L, Chuttani R, et al. Sclerosing agents for use in GI endoscopy. GastrointestEndosc2007;66:1-6. doi:10.1016/j.gie.2007.02.014.

  43. Antacids Alice (Siyue) Li 2015 PharmD Candidate Purdue College of Pharmacy

  44. Indications • Relieve heartburn, sour stomach, or acid indigestion • Some contain simethicone, which may relieve the symptoms of excess gas How do they work? • Neutralizing excess stomach acid • Simethicone lower the surface tension of gas bubbles

  45. Contraindications • Aluminum-containing antacids • Hypersensitivity • Caution in HF, renal failure, edema, recent GI bleed • Magnesium-containing antacids • Hypersensitivity • Extreme caution in myasthenia gravis or other neuromuscular disease, renal impairment • Calcium-containing antacids • Hypersensitivity • Caution in renal impairment, hx of kidney stones, hypoparathyroiddisease, achlorhydria • Sodium bicarbonate-containing antacids • Alkalosis, hypernatremia, severe pulmonary edema, hypocalcemia, unknown abdominal pain

  46. Possible Adverse Effects • Aluminum-containing antacids • Constipation, discoloration of feces (white speckles), fecal impaction, N/V, stomach cramps • Magnesium-containing antacids • Diarrhea, N/V, dizziness, fatigue, electrolyte disturbances • Calcium-containing antacids • Constipation, bloating, gas, hypercalcemia, headache, acid rebound, N/V anorexia, electrolyte disturbance • Milk-alkali syndrome with very high, chronic dosing +/- renal failure • Sodium bicarbonate-containing antacids • Belching, flatulence, gastric distension, tetany, • Metabolic alkalosis, hypernatremia, hypocalcaemia • Milk-alkali syndrome especially with renal dysfunction • CHF exacerbation, edema, cerebral hemorrhage,

  47. Antispasmodics Belladonna alkaloids, Donatal (hyoscyamine, atropine, scopolamine, phenobarbitol), Librax (clidinium, chlordiazepoxide)

  48. Indications • Adjunct in treatment of irritable bowel syndrome, acute enterocolitis, duodenal ulcer How do they work? • Anticholinergic agents inhibit the muscarinic actions of acetylcholine at the postganglionic parasympathetic neuroeffector sites, including smooth muscle, secretory glands, and CNS sites.

  49. Contraindications • Donatal • Narrow angel glaucoma, GI/GU obstruction, myasthesia gravis, paralytic ileus, intestinal atony; unstable cardiovascular status in acute hemorrhage; severe ulcerative colitis (especially complicated by toxic megacolon); hiatal hernia associated with reflux esophagitis; acute intermittent porphyria; restlessness and/or excitement caused by phenobarbital • Librax • Hypersensitivity, glaucoma, prostatic hyperplasia, benign bladder neck obstruction • Anticholinergic agents – avoid in geriatric patients • Caution in patients with impaired renal/liver function, impaired gag reflex, depression, hx of drug abuse and respiratory disease

  50. Possible Adverse Effects http://media-cache-ec0.pinimg.com/236x/42/61/9d/42619d447565cbd965164810fd615763.jpg

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