NCM-106-mod-5-9-study-guide (2) PDF Study Guide

PHARMACOLOGY LECTURE | 2ND YEAR 1ST SEMESTER Garcia, D. MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS PHASES OF RESPIRATION OUTLINE...

PHARMACOLOGY LECTURE | 2ND YEAR 1ST SEMESTER Garcia, D. MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS PHASES OF RESPIRATION OUTLINE Ventilation is the phase in which oxygen passes through the airways TOPIC o Inspiration o Expiration SUBTOPIC I o Perfusion involves blood flow at the alveolar SUBTOPIC II capillary bed. Perfusion is influenced by alveolar pressure. For gas exchange to occur, the perfusion UNDER SUBTOPICS of each of the alveolus must be matched by adequate ventilation o Diffusion the movement of molecules from higher to IMPORTANT / MUST REMEMBER lower concentration; takes place when oxygen passes through the capillary bed to be circulated Additional notes and carbon dioxide leaves the capillary bed and diffuses into the alveoli for ventilator excretion Matched by adequate ventilation otherwise known as VQ, ventilation perfusion ratio. REVIEW OF RESPIRATORY SYSTEM The Respiratory tract is divided into two major parts: UPPER RESPIRATORY DISORDERS o The Upper Respiratory Tract Common Colds (most prevalent) Everything o Caused by rhinovirus and affects primarily the above the nasopharyngeal tract. trachea o Most contagious 1 to 4 days before the onset of symptoms (incubation period) and during the last 3 days of the colds. o Symptoms include: rhinorrhea (watery nasal discharge); nasal congestion, cough and increased mucosal secretions Typical “Sip-on or Kataro” Nasopharyngeal – from the nose down to throat area Acute rhinitis o Acute inflammation of the mucus membranes of the nose, usually accompanies the common cold. Rhino – more on the nose o Lower Respiratory Tract Sinusitis Sinusitis – more of sinuses (frontal, ethmoid, maxillary) Acute pharyngitis (Sore throat) Sore throat doesn’t necessary mean na may tonsilitis, sore throat is inflammation of pharyngeal area THE GROUP OF DRUGS USED TO MANAGE COLD SYMPTOMS Antihistamines (H1 blockers) Decongestants (sympathomimetric amines) Antitussives (anticough) Expectorants RESPIRATION AND VENTILATION Ventilation o The movement of air from the atmosphere through These drugs can be used singly or in combination preparations the upper and lower airways to the alveoli Respiration o Process of gas exchange in the alveolar capillary ANTIHISTAMINES (H1 BLOCKERS OR H1 ANTAGONIST) membrane suppress the histamine-induced wheal response (swelling) and flare response (vasodilation) by blocking You can well-ventilated but poor respiration or vice versa. You can the binding of histamine to its receptors or reducing have a proper respiratory function but has poor ventilation (room histamine receptor activity on nerves, vascular smooth has no air muscle, glandular cells, endothelium, and mast cells. intake, or Prevent histamine to go on with its process too hot) FIRST – GENERATION ANTIHISTAMINES Can cause drowsiness, dry mouth and other anticholinergic symptoms Can cause CNS depression if taken with alcohol, narcotics hypnotics, and barbiturates. Examples: o Diphenhydramine PATATASLAMANG 1  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS o Chloramphenicol Side Effects: o Jittery, nervous, or restless (decrease or disappear SECOND-GENERATION ANTIHISTAMINES as the body adjusts to the drug) Fewer anticholinergic effects and a lower incidence of o Rebound nasal congestion drowsiness o Increase blood pressure and glucose level Examples: o Cetirizine That’s why if the physician’s order is only for 5 days or 7 days, do o Claritin not go beyond that otherwise rebound nasal congestion will happen. When you give a medication, you stop or stimulate ADVERSE EFFECT OF ANTIHISTAMINE INCLUDES TACHYCARDIA something in the system of a person. The system of that person will This happens because when you have a non-inflammatory process, always try to balance off or compensate. When you give too much blood vessels dilate. Once it dilates, the heart compensates or lack can cause secondary effect. pressure. That is why the heart is secondary compensation causing tachycardia in some cases. Drug Interactions: o Pseudoephedrine may decrease the effect of beta blockers. CHOLINERGIC o Hypertension or cardiac dysrhythmias if take with MAOI’s (monoamine oxidase inhibitors) substance is capable of producing, altering, or releasing o Coffee and tea can increase restlessness and acetylcholine, or butyrylcholine ("indirectacting"), or palpitations. mimicking their behaviours at one or more of the body's acetylcholine receptor ("direct-acting") or butyrylcholine receptor types ("direct-acting"). INTRANASAL GLUCOCORTICODS Side effects Effective for treating allergic rhinitis because they have o Dry mouth. an inflammatory action, thus decreasing the allergic o Blurred vision. rhinitis symptoms of rhinorrhea, sneezing and congestion o Dry eyes. Examples: o Constipation. o Beclomethasone o Urinary retention. o Budesonide o Dizziness due to drop in blood pressure on standing o Dexamethasone up (postural hypotension) o Flunisolide o Cognitive problems (confusion) o Fluticasone o Heart rhythm disturbance. o Mometasone o Triamcinolone Ending with -sone Intranasal glucocorticoids undergo rapid deactivation after absorption. Most allergic rhinitis is seasonal; therefore the drugs are for short-term use unless otherwise indicated by the health care provider ANTITUSSIVES Act on the cough-control center in the medulla to suppress the cough reflex. The cough is a naturally protective way to clear the airway of secretions or any collected material. Sore throat may cause coughing that increases throat irritation. If the cough is non-productive and irritating, an antitussive may be taken. 3 TYPES OF ANTITUSSIVES Non – Opioid o Dextromethorphan HBr Opioid o Codeine Combination o Paracetamol + Phenylephrine HCl + NASAL AND SYSTEMIC DECONGESTANTS Dextromethorphan HBr o Tusedex Nasal congestion results from dilation of nasal blood vessels caused by infection, inflammation or allergy. Side effects of opioids: respiratory depression, respiratory rate With this dilation, the transudation of fluid into the tissue spaces occurs that results in swelling of the nasal cavity. decreases Nasal decongestants stimulates the alpha adrenergic receptors, producing vascular constriction (vasoconstriction) of the capillaries within the nasal EXPECTORANTS mucosa. The result is shrinking of the nasal mucous Stimulates the airways to expel mucus in the respiratory membranes and a reduction in fluid secretion tract Nasal decongestants are administered by nasal spray or Example: drops or in tablet, capsule or liquid form. Frequent use of o Guaifenesin decongestants, especially nasal spray or drops, can In order to remember the example of expectorant, gua means result in tolerance and rebound nasal congestion. “paguwa” to put out Recommended for those who have pneumonia or upper tract SYSTEMIC DECONGESTANTS infection Examples: o Ephedrine o Phenylephrine Synergestic Effect – two medications combined to form an even o Oxymetazoline and greater function o Pseudoephedrine PATATASLAMANG 2  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS Example is dextromethorphan (antitussive) and guaifenesin Administered by inhalation only with the HandiHaler (expectorant) combined together they help thin out mucus and device (dry-powder capsule inhaler) prevent coughing. Then, when the mucus thin outs, it will go HandiHalers should be washed with warm water and along the circulatory system, and it would make it easy to put dried. out. Side Effects: o dry mouth o constipation MUCOLYTICS o vomiting Act as detergents to liquefy and loosen thick, mucous o dyspepsia secretions so that they can be expectorated o abdominal pain Examples: o depression o Carbocisteine o insomnia o Acetylcysteine o headache o Bromhexine o joint pain o peripheral edema. LOWER RESPIRATORY TRACT DISORDERS IPRATOPIUM BROMIDE Chronic obstructive pulmonary disease (COPD) and Used tp treat asthmatic conditions by dilating the restriction pulmonary disease are the two major bronchioles. categories of lower respiratory tract disorders. Fewer systemic effects. COPD is caused by airway obstruction with increased Administered by MDI airway resistance of airflow to lung tissues. Note: Ipratropium with albuterol sulphate is used to treat Four major pulmonary disorders: COPD. o Chronic bronchitis Cholinergic – parasympathetic, parasympathetic response is o Bronchiectasis bronchoconstriction, so you give you anticholinergic o Emphysema o Asthma By practice, usually ipratropium bromide is combines with Chronic bronchitis, bronchiectasis, and emphysema salbutamol to decrease the palpitation when they used nebulizer frequently result in irreversible lung tissue damage. The lung tissue changes that result from an acute asthmatic attack are normally reversible; however, if the attacks are METHYLXANTHINE (XANTHINE) DERAVATIVES frequent and asthma becomes chronic, irreversible Relaxes the smooth muscles of the bronchi, bronchioles changes in the lung tissue may result. and pulmonary blood vessels by inhibiting the enzyme phosphodiesterase, resulting in an increase in cAMP, MEDICATIONS FREQUENTLY PRESCRIBED FOR COPD which promotes bronchodilation. Bronchodilators Toxicity to occur when the serum level is greater than 20 o Used to assist in opening narrowed airways. mcg/ml. Inhalers – fastest drug route Half life if affected by age of patient Glucocorticoids (steroids) Examples: o Used to decreased inflammation. o Theophylline Watch out for sugar (glucose) o Aminophylline o Caffeine Leukotriene modifiers Side effects and adverse effects: o Reduce inflammation in the lung tissue o Anorexia Cromolyn o nausea and vomiting o Acts as an inflammatory agent by suppressing the o gastric pain caused by increased gastric acid release of histamine and other mediators from the secretion mast cells. o intestinal bleeding Expectorants o nervousness o Used to assist in loosening mucus from the airways. o dizziness Antibiotics o headache o May be prescribed to prevent serious complications, o irritability from bacterial infections o cardiac dysrhythmias o tachycardia SYMPATHOMIMETICS: ALPHA AND BETA2 ADRENERGIC AGENTS o palpitations Examples: o marked hypotension o Albuterol (more selective for Beta2 receptors) o hyperreflexia o Metoproterenol o seizures Albuterol only available in US, PH equivalent Salbutamol Rapid IV administration of aminophylline, can cause Can be administered orally or by inhalation with a dizziness, flushing, hypotension, severe bradycardia, metered-dose inhaler and palpitations. To avoid severe adverse effects, IV Onset of action: Theophylline preparations must be administered slowly o 1 minute by oral inhalation or 5 to 30 minutes by via infusion pump. nebulisation, and 15 to 30 minutes when taken Drug Interactions orally. o Beta-blockers, cimetidine, propanolol and Note: Excessive use of the aerosol drug can lead to erythromycin decrease the liver metabolism rate and tolerance and loss of drug effectiveness. increase the half-life and effects of theophylline. Side effects: o Barbiturates and carbamazepine decrease it’s o Tremors effects. o Headache o Increases the risk of digitalis toxicity and decrease o Nervousness the effects of lithium. o Increased pulse rate o Palpitations (high dosage) Palpitations happen because it is an adrenergic (alpha and beta). In Alpha, Beta1 (heart), Beta2 (lungs), heart will be tachycardic ANTICHOLINERGICS TIOTROPIUM Used for maintenance treatment of bronchospasms PATATASLAMANG 3  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS A combination inhalation drug containing the glucocorticoid fluticasone propionate and salmeterol is effective in controlling asthma symptoms by alleviating airway constriction and inflammation. Side effects: o Throat irritation, hoarseness, dry mouth, coughing, headache, euphoria, confusion, sweating, hyperglycemia, insomnia, nausea, vomiting, weakness and menstrual irregularities. Adverse effects: o Depression, peptic ulcer, loss of bone density, and development of osteoporosis and psychosis. LEUKOTRIENE (LT) INHIBITORS Leukotriene is a chemical mediator that can cause inflammatory changes in the lungs The cysteinyl leukotrienes promote an increase in eosinophil migration, mucous production and airway wall edema that results in bronchoconstriction. Eosinophil – part of blood which increases when there is an allergy CROMOLYN SODIUM or inflammation, so LT inhibitors prohibits this process Is used for prophylactic treatment of bronchial asthma, and it must be taken daily. LT modifiers are effective in reducing inflammatory symptoms of asthma triggered by allergic and It is not used for acute asthmatic attack. environmental stimuli. Cromolyn does not have bronchodilator properties but ZAFIRLUKAST instead act by inhibiting release of histamine and other inflammatory mediators from mast cells to prevent Reduce the inflammatory process and decrease asthma attack. bronchoconstriction. It can be used with beta adrenergic and xanthine Administered orally derivatives Moderately long half-life The drug should not be discontinued abruptly because a rebound asthmatic attack can result ZILEUTON Side effects: Short half-life of 1 to 2.3 hours o Postnasal drip o Irritation of the nose and throat MONTELUKAST o Cough o These effects can be decreased by drinking water Short half-life of 2.7 to 5.5 hours before and after using the drug. Safe for children 2 years and older. Adverse effects: o Rebound bronchospasm ANTIMICROBIALS Are used only if a bacterial infection results from retained mucous secretions. Trimethoprim-sulfamethoxazole is effective for the treatment of mild to moderate acute exacerbation of chronic bronchitis (AECB’s) from infection causes. Whenever the px is asthmatic or allergic, do not start automatically GLUCOCORTECOIDS (STEROIDS) with antibiotic. You need to find how it started. Has anti-inflammatory action and are indicated if asthma GASTROINTESTINAL TRACT DRUGS is unresponsive to bronchodilator therapy or if the patient GASTROINTESTINAL TRACT DISORDERS has an asthmatic attack while on maximum doses of Vomiting theophylline or an adrenergic drug. Diarrhea Can be given using the following methods: Constipation o MDI inhaler – Beclomethasone Drugs groups used to correct or control vomiting, o Tablet – Dexamethasone, prednisone, prednisolone, diarrhea, and constipation are classified as antiemetics, methylprednisolone emetics, antidiarrheals and laxatives. o Intravenous – Dexamethasone Vomiting (emesis) Inhaled glucocorticoids are more effective for controlling o the expulsion of gastric contents, has a multitude of symptoms of asthma than are bete2 agonist, particularly causes, including motion sickness, viral and in reduction of bronchial hyperresponsiveness. bacterial infection, food intolerance, surgery, Always gargle after using inhalers because the medication left in pregnancy, pain, shock, effects of selected oral mucosa may cause fungal infection drugs(e.g., antineoplastics, antibiotics) radiation, Inhaled glucocorticoids are preferred over oral disturbance of the middle ear that affect equilibrium. preparations unless they fail to control the asthma Nausea Examples: o a queasy sensation, may or may not precede the o Prednisone expulsion. o Prednisolone Antiemetics can mask the underlying cause of vomiting o Dexamethasone and should not be used until the cause has been ▪ For management of moderate to severe asthma determined, unless the vomiting is so severe as to cause exacerbations. dehydration and electrolyte imbalance. o Methylprednisolone The two cerebral centers o the chemoreceptor trigger zone (CTZ) PATATASLAMANG 4  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS ▪ which lies near the medulla, o Drowsiness o The vomiting center in the medulla o Dryness of mouth ▪ cause vomiting when stimulated. o Constipation The CTZ BISMUTH SUBSALICYLATE receives most of Acts directly on the gastric mucosa to suppress vomiting. the impulses from They are marketed in liquid or chewable tablet forms and the drugs, toxins, can be taken for gastric discomfort or diarrhea. and the vestibular center in the ear PHOSPHORATED CARBONATED SOLUTION and transmits them A hyperosmolar carbohydrate, decreases nausea and to the vomiting vomiting by changing the gastric pH. center. The It may also decrease the smooth muscle contraction of neurotransmitter the stomach dopamine Patient with diabetes mellitus should avoid this drug stimulates the because of its high sugar content CTZ, which in turn stimulates the ANTIHISTAMINES AND ANTICHOLINERGICS vomiting center. When the vomiting center is stimulated, the motor neuron responds by causing contraction of the Acts primarily on the vomiting center; they also act by diaphragm, the anterior abdominal muscles, and the decreasing stimulation of the CTZ and vestibular stomach. The glottis closes, the abdominal wall moves pathways. upward, and vomiting occurs. Only a few prescription antihistamines and anticholinergics are used in the treatment of nausea and Non-pharmacologic measures should be used first when vomiting. nausea and vomiting occur. Side effects If non-pharmacologic measures are not effective, o drowsiness, which can be a mojor problem antiemetics are combined with nonpharmacologic o dry mouth measures. o blurred vision, caused by papillary dilation o tachycardia (with annticholinergic use), o constipation These drugs should not be used by patient with glaucoma Example of Antihistamine: o Hydroxyzine – post-operative nausea and vomiting Usually attacks the post-vomiting area of the brain Example of Anticholinergic o Scopolamine – motion-sickness Transdermal patch DOPAMINE ANTAGONIST Suppresses emesis by blocking dopamine (D2) Burnt toast – to stimulate your vagus response in order to inhibit receptors in the CTZ your vomiting reflexes PHENOTHIAZINES ANTIEMETICS Tea has the component called Tannic acid to prevent vomiting, inhibits you to feel that salty or oily Used to treat nausea and vomiting resulting from Soda – others if they can’t drink softdrinks, they feel like vomiting. surgery, anesthetics, chemotherapy, and radiation sickness. The carbonated content of the soda helps in burping which opens They act by inhibiting the CTZ. the airway and gastro pathway Have antihistamines and anticholinergic properties Mainly used as antipsychotic TWO MAJOR GROUPS OF ANTIEMETICS Examples: Nonprescription o Chlorpromaine o Antihistamines o Prochlorperazine edisylate o Bismuth subsalicylate, o Promethasine (High-alert medication) o Phosphorated carbohydrate solution Side Effects: Prescription o moderate sedation o Antihistamines o hypotension o Dopamine antagonist o extrapyramidal symptoms o Benzodiazepine o CNS effects (restlessness, weakness, dystonic o Serotonin antagonist reactions, agitation) o Glucocorticoids Because the dose is lower for vomiting than for o Cannabinoids psychosis, the side effects are not so severe. o Miscellaneous antiemetics BUTYROPHENONES ANTIHISTAMINE ANTIEMETICS Block the D2 receptors in the CTZ. They are used to treat postoperative nausea and Examples: o Dimenhydrinate vomiting and emesis associated with toxins, cancer o Cyclizine hydrochloride chemotherapy and radiation therapy o Meclizine hydrochloride Mainly used as antipsychotic o Diphenhydramine hydrochloride Examples: Can be purchased without a prescription to prevent o Haloperidol nausea, vomiting, and dizziness (vertigo) caused by o Droperidol motion. These drugs inhibit vestibular stimulation in the middle SEROTONIN RECEPTOR ANTAGONIST ear. Suppresses nausea and vomiting by blocking the Diphenhydramine is also used to prevent or alleviate serotonin receptors in the CTZ and blocking the afferent allergic reactions to drugs, insects, and food by acting as vagal nerve terminals in the upper GI tract an antagonists to histamine 1 (H1) receptors Side effects: PATATASLAMANG 5  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS Are the most effective of all antiemetics in suppressing patient with severe hepatic impairment should not take nausea and vomiting caused by cancer chemotherapy- products that contain dyphenoxilate, difenoxin, and induced emesis loperamide Examples: o Ondansetron ABSORBENTS o Granisetron Act by coating the wall of the GI tract and adsorbing o Dolasetron bacteria or toxins that cause diarrhea o Palonesetron Examples Ends with tron o Kaolin CANNABINOIDS o Pectin Alleviate nausea and vomiting resulting from cancer o Colestipol treatment. o Cholestyramine MISCELLANEOUS ANTIEMETICS CONSTIPATION Trimethobenzamide – suppresses impulses to the CTZ. Constipation, the accumulation of hard fecal material in Metoclopramide – suppresses emesis by blocking the the large intestine, is a relatively common complaint and dopamine receptors in the CTZ. a major problem for older adults. Insufficient water intake Metoclopramide – aside suppressing the emetic center, it lets your and poor dietary habits are contributing factors. In older adults, the GI motility is decreased that is why the fecal GI tract move so that the food will not stay in gastric mucosa matter doesn’t move resulting to clumping up decreasing the stimulation of vomiting reflex Other causes include DIARRHEA o Fecal impaction Diarrhea, frequent liquid stool, is a symptom of an o Bowel obstruction intestinal disorder. o Chronic laxative use Causes include o Neurologic disorders (paraplegia) o Foods (spicy, spoiled) o Ignoring the urge to defecate o Fecal impaction o Lack of exercise o Bacteria (Escherichia coli, Salmonella) or viruses o Select drugs such as anticholinergics, narcotics, and (parvovirus, rotavirus), certain antacids o Toxins Nonpharmacologic Measures o Drug reactions o Diet (high fiber) o Laxative abuse o Water o Malabsorption syndrome caused by lack of digestive o Exercise enzymes o Routine bowel habits o Stress and anxiety o A ‘’normal’’ number of bowel movements ranges o Bowel tumor between one and three per day to three per week. o Inflammatory bowel disease such as ulcerative LAXATIVES AND CATHARTICS colitis or Crohn disease. Are used to eliminate fecal matter Nonpharmacologic Measures Laxatives promote a soft stool. o The cause of diarrhea should be identified. o Nonpharmacologic treatment for diarrhea is Cathartics result in a soft to watery stool with some recommended until the underlying cause can be cramping. determined. Side effect: they are GI irritants o This includes use of clear liquids and oral solutions 4 types of laxatives: such as Gatorade (for adults) and Pedialyte or o Osmotics (saline) Rehydralyte (for children) and IV electrolyte o Stimulants (contact or irritation) solutions. o Bulk-forming Sugar content of Gatorade is high which causes irritation in the GI o Emollients (stool softeners) tract that leads in even more diarrhea which can reach to the OSMOTICS (HYPEROSMOLAR LAXATIVES) phase where the GI tract cannot control the too much sugar that Include salt or saline products that consist of sodium or tend to osmotic diarrhea magnesium. o Anti-diarrheal drugs are frequently used in Hyperosmolar salts pull water into the colon and combination with nonpharmacologic treatment increase water in the feces to increase bulk, which Traveler’s Diarrhea stimulates peristalsis. o Travelers’ diarrhea, also called acute diarrhea, is Good renal function is needed to excrete any excess usually caused by E.coli. It ordinarily lasts less than salts. 2 days; however, if it becomes severe, Saline cathartics are contraindicated for patients with fluoroquinolone antibiotics are usually prescribed. heart failure. Loperamide may be used to slow peristalsis and Examples: decrease the frequency of defecation, but it can also o Sodium salts (sodium phosphate or Phospho-Soda, slow the exit of organism from the GI tract. sodium biphosphate) Travelers’ diarrhea can be reduced by drinking o Magnesium salts (magnesium hydroxide or Milk of bottled water, washing fruit, and eating cooked magnesia, magnesium citrate) vegetables o Polyethylene glycol (PEG) (used for bowel pprepartion for diagnostics and surgical procedure) ANTIDIARRHEALS o Lactulose – not absorbed, draws water into the OPIATES AND OPIATE-RELATED AGENTS intestines to form a soft stool. o Glycerin Opiates decrease intestinal motility thereby decreasing Lactulose fluid – Gatorade peristalsis. Milk of magnesia – to stimulate defecation and movement of GI Opium antidiarrheals can cause CNS depression when tract but watch out when giving as it contains magnesium so if the taken with alcohol, sedatives and tranquilizers. Examples: px has renal failure, check the magnesium level o Diphenoxylate with atropine (frequently prescribed with travellers’ diarrhea) STIMULANT (CONTACT) LAXATIVES o Difenoxin with atropine (treat nonspecific and Increase peristalsis by irritating sensory nerve endings in chronic diarrhea) the intestinal mucosa. o Loperamide Examples: PATATASLAMANG 6  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS o Bisacodyl – used to empty the bowel before diagnostic test. o Senna o Castor oil – harsh laxative (purgative) that acts on the small bowel and produces a watery stool. Not FDA approved to correct constipation but rather it is used mainly for bowel preparations. Side effects: o Nausea o abdominal cramps o weakness o reddish brown urine caused by excretion of phenolphthalein, senna or cascara BULK-FORMING LAXATIVES Are natural fibrous substances that promote large, soft stools by absorbing water into the intestines, increasing TRANQUILIZERS the fecal bulk and peristalsis. Have minimal effect in preventing and treating ulcers; Non-absorbable however, they reduce vagal stimulation and decrease Defecation usually occurs 8 to 24 hours anxiety. Examples: A combination of anxiolytic and anticholinergic may be o Polycarbophil used in treating ulcers: o Polyethylene glycol o Chlordiazepoxide (anxiolytic) o Methylcellulose o Clidinium bromide (anticholinergic o Psyllium Side effects: Side effects: o Edema o Nausea o Ataxia o Vomiting o Confusion o flatus or diarrhea may occur if taken excessively. o EPS Fiber-rich foods – bread, rice, corn, vegetables o Agranulocytocis CHLORIDE CHANNEL ACTIVATORS ANTICHOLINERGICS (ANTIMUSCARINICS, PARASYMPATHOLYTICS) New category of laxatives used to treat idiopathic constipation in adults. These drugs relieve pain by decreasing GI motility and Example: secretion. o Lubiprostone – activates calcium channel in the They act by inhibiting acetylcholine and blocking small intestines, leading to an increase in intestinal histamine and hydrochloric acid. fluid secretion and motility. Delay gastric emptying time, so they are used more Adverse effect: frequently in duodenal ulcers than for gastric ulcers. o nausea that seems to be dose dependent Examples: o diarrhea o Propantheline bromide – inhibits gastric acid o headache secretions in the treatment of peptic ulcers. o abdominal distention and flatulence. o Glycopyrrolate – for duodenal ulcer Idiopathic – unknown cause should be taken before meals to decrease acid secretion that occurs with eating. EMOLLIENTS Antacids can slow down the absorption of Are lubricants and stool softener (surface-acting or anticholinergics and therefore should be taken 2 hours wetting drugs). after anticholinergic administration. ANTACIDS Decrease straining during defecation. Examples: Promotes ulcer healing by neutralizing hydrochloric acid o Mineral oil – increases water retention in the stool. and reducing pepsin activity. Absorbs fat-soluble vitamins, ADEK. They do not coat the ulcer. o Docusate calcium 2 types of antacids: o Dosusate sodium o Systemic effect Mineral oil can be given through intrarectal and oral o non-sytemic effect Example of Systemic effect: ULCER o Sodium bicarbonate Peptic Ulcer is a broad term for an ulcer that occurs in Side effects: the esophagus, stomach, or duodenum within the upper o Sodium excess (causing hypernatremia and water GI tract. retention) The classic symptom of peptic ulcers is gnawing, aching o Metabolic alkalosis caused by excess bicarbonate abdominal pain o Acid rebound (excess acid secretion) Calcium carbonate ANTIULCER DRUGS o most effective in neutralizing acid o can cause rebound acid Tranquilizers – decrease vagal activity Examples Non-systemic Anticholinergics – decrease acetylcholine by blocking the o Aluminium hydroxide cholinergic receptors o Magnesium hydroxide Antacids – neutralize gastric acid o Magnesium trisilicate H2 blockers – block the H2 receptors Side effects: PPI’s – inhibit gastric acid secretion o Magnesium compounds – diarrhea Pepsin-inhibitor sucralfate o Aluminum and calcium - constipation Prostaglandin E1 analogue misoprostol - inhibits gastric Antacids that contains magnesium salts are acid secretion and protects mucosa contraindicated in patients with impaired renal function Misoprostol – general name of Cytotec, used for unwanted babies because it is of the risk for hypermagnesemia (abortion) Magnesium compound – “magneshhhhh” diarrhea Aluminum and calcium – “aluuumm” constipation PATATASLAMANG 7  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS HISTAMINE2 BLOCKERS Antitussives agents are used primarily in: Are popular drugs used in the treatment of gastric and - Nonproductive coughs duodenal ulcers. Antitussive agents are used to: These drugs block the H2 receptors of the parietal cells - Prevent a cough from developing in the stomach thus reducing gastric acid secretion and Common side effects caused y antihistamines include: concentration - GI upset Examples: For which of the following patients would giving o Cimetidine – has a short half-life and a short antitussives be contraindicated duration of action; blocks about 70% of acid - 54 year old male with allergy to secretion for 4 hours. dextromethorphan o Ranitidine – has longer duration of action (up to 12 The adverse reaction most commonly associated with hours) than cimetidine. antihistamine is o Famotidine - is 50% to 80% more potent than - Tachycardia cimetidine and is to five to eight times more potent The main action of sympathomimetric bronchodilators is than ranitidine. It is indicated for short-term use (4 to to: 8 weeks) for duodenal ulcer and for Zollinger-Ellison - Relax the smooth muscles of the bronchi syndrome. The half-life of xanthine bronchodilators is influenced by o Nizatidine – is an H2 blocker that can relieve which of the following specific factors? nocturnal gastric acid secretion for 12 hours - Age of patient To prevent recurrence of duodenal ulcers, administer The primary action of antidiarrheals is to: nizatidine 150 mg twice a day at bedtime or famotidine - Reduce the irritability of the bowel and reduce 20 mg twice a day at bedtime. the motility of the GI tract 50% to 80% of Cimetidine is excreted unchanged in the What are the most common adverse reactions that can urine. It can also cause an increase in BUN, serum occur with all laxatives? creatinine, and serum alkaline phosphatise - Abdominal cramps and diarrhea Ranitidine, famotidine and nizatidine also promote Which drug classifications are used to treat both diarrhea healing of the ulcer by eliminating it’s cause. Their and increased bowel motility? duration of action is longer, decreasing the frequency of - Antidiarrheal dosing, and they have fewer side effects and fewer drug Antidiarrheal medications are important to control interaction than cimetidine.’ diarrhea which, if prolonged can lead to: - Dehydration PEPSIN INHIBITORS (MUCOSALL PROTECTICE DRUGS) How many antacids can be associated with Example hypermagnesemia o Sucralfate - a complex of sulfated sucrose and - They contain magnesium aluminum hydroxide, is classified as a pepsin Caster oil is an example of what type of laxative? inhibitor, or mucosal protective drug. It is - Stimulant nonabsorbable and combines with protein to form a Why might laxatives that contain sodium be viscous substance that covers the ulcer and protects contraindicated in a patient with a chronic heart failure? it from acid and pepsin. This drug does not - They can lead to an exacerbation of cardiac neutralize acid or decrease acid secretions symptoms The primary use of anticholinergic- antispasmodic agents is to treat: - Peptic ulcer Which antacid is the drug of choice for treatment of peptic ulcer disease? - Esomeprazole You are reviewing an order for metoclopramide (Reglan) for your patient. Which order would you need to clarify prior to giving? - Reglan 10 mg orally at bedtime Which major groups of laxative is useful for patients who should not strain while having bowel movement? - Stool softeners and saline laxatives Frank, age 84, comes to the clinic with mild abdominal discomfort, increased flatus, and watery stools. His QUIZ history includes mild prostatic hypertrophy. Mr. Frank Cromolyn sodium is a medication used for should be started on which GI medications to treat his - Prophylaxis of asthma attacks diarrhea? Histamine, a chemical produced by the body: - Azulfidine - Produces the inflammatory response in the If the patient is taking an anticoagulant, which H2 body histamine blocker if the medication most likely to The 2 major types of bronchodilators are: interfere with the anticoagulant? - Beta2 adrenergics and anticholinergic - Cimetidine Narcotic antitussives acts by: Your patient who is starting on a proton pump inhibitor - Suppressing the cough reflex by acting directly (Protonix) asks you when would be the best time for her on the cough center in the brain to take the medication. Your response will be: Antihistamines act to competitively block the action of: - You should take your protonix before meals - Histamine by producing vasodilation and Which drug is one of the bulk-forming laxative? increased capillary permeability - Citrucel Aminophylline is an important agent to use to determine if the patient has bronchospasms or pulmonary edema. This agent is in the drug family of: - Xanthin bronchodilators Leukotriene receptor inhibitors are used primarily to: - Reduce inflammation Drugs that are known to interact with leukotriene receptor inhibitors includes all of the following except: - Theophylline PATATASLAMANG 8  MODULE 5: RESPIRATORY AND GI SYSTEM DRUGS PATATASLAMANG 9 PHARMACOLOGY LECTURE | 2ND YEAR 1ST SEMESTER Garcia, D. MODULE 7: ENDOCRINE DRUGS OUTLINE TOPIC SUBTOPIC I SUBTOPIC II UNDER SUBTOPICS IMPORTANT / MUST REMEMBER Posterior pituitary – 2 hormones present (Oxytocin and Additional notes Vasopressin/ADH) Posterior pituitary – only stores the hormones, it does not make its own hormone THE ENDOCRINE SYSTEM PITUITARY GLAND AGENTS (ANTERIOR LOBE/ADENOHYPOPHYSIS The APG secretes hormone that target glands and tissues, including o Growth Hormone (GH) stimulates growth o Thyroid-stimulating hormone (TSH) which acts on the thyroid gland o Adrenocorticotropic hormone (ACTH) which stimulates the adrenal gland o Gonadotropins (Follicle-stimulating hormone) and Luteinizing hormone which affects the ovaries and THE NEGATIVE-FEEDBACK MECHANISM testes. o Prolactin (PRL) which primarily affects the breast tissues GROWTH HORMONE 2 hypothalamic hormones regulate growth hormones o GH-releasing hormone (GH-RH; somatropin) o GH-inhibiting hormone (GH-IH; somatostatin) GH does not have a specific target gland It affects body tissues and bone GH replacement stimulates linear growth when there are GH deficiencies. GH drugs cannot be given orally because they are inactivated by GI enzymes. Subcutaneous (subcut) or intramuscular (IM) administration is necessary GH-Releasing hormone – somatropin Form the target organ, it send signals to the hypothalamus, then GH-inhibiTing hormone - somaTosTaTin the hypothalamus sends releasing hormone to the pituitary. The pituitary will send stimulating hormone to the target organ/gland. SOMATROPIN (DRUG THERAPY: GROWTH HORMONE DEFICIENCY) Once, it will fulfill the target gland, it will send feedback to the Is a GH used to treat growth failure in children because of hypothalamus to stop. In a normal system, the feedback GH deficiency mechanism regulates the amount of hormones (lack or too much). It promotes release of growth hormones Somatropin is a product that has the identical amino acid sequence as human growth hormone (HGH) It is contraindicated in pediatric patients who have growth deficiency due to Prader-Will syndrome and in those who are severely obese or who have severe respiratory impairment because fatalities associated with these factors can occur. PATATASLAMANG 1  MODULE 7: ENDOCRINE DRUGS Drug interactions: Caution: o Corticosteroids can inhibit the effects somatropin o Caution is advised when administering in patients o Can enhance the effects of antidiabetics and can receiving diuretics cause hypoglycemia o Can increase electrolyte loss Side Effects: Side Effects: o Parenthesia (burning or prickling sensation), o Bradycardia arthralgia (joint pain), myalgia (muscle pain), o Hypertension peripheral edema, weakness, and cephalgia (cluster o Sinus tachycardia headache) o Peripheral edema Adverse Reaction: CORTICOTROPIN o Seizures Used to diagnose adrenal gland disorders o Intracranial hypertension Used to treat multiple sclerosis and treat infantile spasms o Secondary malignancy (e.g leukemia) Available as Repository Corticotropin Injection (RCI), Gigantism – excess growth during childhood caused by a administered via IM or subcut pituitary tumor RCI controls the synthesis of ACTH from cholesterol Gigantism – proportional growth which stimulates adrenal glands in releasing it’s hormones Acromegaly – excessive growth after puberty Not proportional, only certain parts gets big PROLACTIN If the tumor cannot be destroyed by radiation GH receptor Stimulation of breast tissue for milk production antagonist, somatostatin analogues or dopamine agonist Hypoprolactinemia – deficiency PRL are given acting by either blocking GH receptor sites or Hyperprolactinemia-excess PRL inhibiting secretion of GH o Males – excess breast tissue (gynecomastia) and may lactate (galactorrhea), decrease sperm SOMASTOSTATIN (DRUG THERAPY: GROWTH HORMONE EXCESS) production. GH receptor antagonist o Females – can experience lactation not pregnancy o Pegvisomant related, amenorrhea. ▪ Blocks GH receptor sites, preventing abnormal Excess PRL can be treated with dopamine agonist growth by normalizing insulin-like growth factor 1 o Bromocriptine (IGH-1) level o Cabergoline – better tolerated, has a longer half-life. ▪ Given injection POSTERIOR LOBE (NEUROHYPHYSIS) AGENTS ▪ Hyperhidrosis (abnormally excessive sweating); The PPG secretes ADH (antidiuretic hormone) and cephalgia and fatigue Oxytocin. ▪ Adverse reaction: chest pain, hypertension, and ADH promotes water reabsorption from the renal tubules elevated hepatic transaminases to maintain water balance in the body fluids. When there Elevated hepatic transaminases means that the liver enzymes and is a deficiency of ADH, large amounts of water are all test for liver are elevated excreted by the kidneys (diabetes insipidus); can lead to Somatostatin analogues severe fluid volume deficit and electrolyte imbalances. o Lanreotide ADH preparations, vasopressin and desmopressin ▪ Has a duration of 28 days after a single injection, acetate can be administered intranasal or by injections. therefore injections are given every 4 weeks ADH is contraindicated in patients with moderate to ▪ Administered deep subcutaneous severe renal disease and in patients with hyponatremia or ▪ Side effects: diarrhea, abdominal pain, nausea, a history of such. vomiting, constipation, weight loss and flatulence Side effects: Dopamine agonist o Hyponatremia o Bromocriptine o Cephalgia (A distinctive syndrome of headaches, ▪ Inhibits the secretion of GH caused by pituitary also known as cluster headache or migrainous adenomas neuralgia). When you have adenomas or masses in the certain parts of your o Dyspepsia body, it affects your physiologic function o Diarrhea ▪ Available in oral forms and has fewer side effects o Nausea ▪ Adverse reaction: cardiac toxicity (hypertension, o Vomiting myocardial infraction, and angina), cerebrovascular toxicity (stroke and seizure), SIADH (SYNDROME OF INAPPROPRIATE ANTIDIURETIC should be discontinued if hypertension occurs to HORMONE) pregnancy (preeclampsia, eclampsia or PIH) When secretion of ADH from the PPG (posterior pituitary gland) is excessive, the most common cause is small cell THYROID-STIMULATING HORMONE carcinoma of the lung. Medications, other malignancies, Stimulates the Thyroid gland to release thyroxine (T3) and and stressors (pain, infection, anxiety, trauma) may also triiodothyronine (T4). be causative factors. These conditions lead to an excessive amount of water THYROTROPIN retention expanding the intracellular and intravascular A purified extract of TSH for thyroid cancer volume. Used as a diagnostic agent to differentiate between This increased fluid volume causes enhanced glomerular primary and secondary hypothyroidism filtration and decreased tubular sodium reabsorption. Side Effects: SIADH can be treated by fluid restrictions, by hypertonic o Symptoms of hyperthyroidism (nervousness, anxiety, saline or by drugs such as: demeclocycline, conivaptan, and irritability, sensitivity, palpitations) tolvaptan o Urticaria (Hives), rash, pruritus, and flushing DEMOCLOCYCLINE ADENOCORTICOTROPIC HORMONE (ACTH) Is a tetracycline antibiotic. COSYNTROPIN Adverse effect: o Photosensitivity A synthetic ACTH, is only approved for diagnostic o Dental discoloration purposes and is less potent and less allergenic than o Enamel hypoplasia corticotrophin Fluid and electrolytes must be monitored closely. Stimulates the production and release of cortisol, corticosterone, and androgens from the adrenal cortex Administered via IM and IV VAPTANS (CONIVAPTAN AND TOLVAPTAN) PATATASLAMANG 2  MODULE 7: ENDOCRINE DRUGS Vasopressin receptor antagonists and are indicated for pregnancy can cause hypothyroidism in fetus or the treatment of euvolemic hyponatremia in SIADH. infant. Tolvaptan is given orally. It has black-box warnings for patients with alcoholism, hepatic disease and PARATHYROID GLANDS malnutrition; should be avoided in these patients. The parathyroid glands secrete parathyroid hormone Vaptans are contraindicated in patients with hypovolemia. (PTH), which regulates calcium levels in the blood. Fluid restrictions should be avoided during therapy to A decrease in serum calcium stimulates the release of prevent too rapid an increase in serum sodium. PTH. Calcitonin decreases serum calcium levels by promoting THYROID DRUGS renal excretion of calcium Thyroid controls the metabolism FOR HYPOTHYROIDISM HYPOPARATHYROIDISM Parathyroid hormone agents treat hypoparathyroidism. LEVOTHYROXINE SODIUM Hypocalcemia (serum calcium deficit) can be caused by PTH deficiency, vitamin D deficiency, renal impairment, or Drug of choice for the treatment of primary diuretic therapy, and PTH replacement helps correct the hypothyroidism. calcium deficit. The action of PTH is to promote calcium It increases the levels of T4 and metabolically is absorption from the GI tract, promote reabsorption of deiodinated to T3. calcium from the renal tubules, and activate vitamin D. Used to treat simple goiter and chronic lymphocytic Calcitriol is a vitamin D analogue that promotes calcium thyroiditis (Hashimoto’s disease) absorption from the GI tract and secretion of calcium from bone to the bloodstream LIOTHYRONINE SODIUM Is a synthetic T3 with a biologic half-life of 2.5 days with HYPERPARATHYROIDISM rapid onset of action. Hyperparathyroidism can be caused by malignancies of Is indicated for use as replacement or supplemental the parathyroid glands or ectopic PTH hormone secretion treatment for hypothyroidism of any aetiology. from lung cancer, hyperthyroidism, or prolonged Does not need to be deionated which increases the immobility, during which calcium is lost from bone. availability for use by the body tissues. Synthetic calcitonin treats hyperparathyroidism. Initial therapy for treating myxedema (hypothyroidism) Inhibits osteoclastic bone resorption decreasing calcium levels Myxedema – hypothyroidism is in severe form ADRENAL GLANDS DESICATED THYROID The adrenal cortex produces two types of hormones, or Is a naturally occurring thyroid hormone from porcine corticosteroids: glucocorticoids (cortisol) and thyroid glands. mineralocorticoids (aldosterone). It contains both levothyroxine sodium and liothyronine Cortisol is secreted by the adrenal glands in response to sodium the hypothalamus-pituitaryadrenal (HPA) axis as a result Used to treat hypothyroidism due to thyroid atrophy, of the feedback mechanism. thyroid hormone deficiency and goiter. o A decrease in serum cortisol levels increases CRF and ACTH secretions, which stimulate the adrenal LIOTRIX glands to secrete and release cortisol. o An increased serum cortisol level exerts the negative feedback mechanism, which inhibits the HPA axis, ANTITHYROID DRUGS resulting in less cortisol being released Reduce the excessive secretion of thyroid hormones by A decrease in corticosteroid secretion is called adrenal inhibiting thyroid secretions. hyposecretion (adrenal insufficiency, or Addison’s Drug of choice are Thiourea derivatives (thioamides) : disease), and an increase in corticosteroid secretion is decreases thyroid hormone production called adrenal hypersecretion (Cushing’s syndrome) Cushing – “cushion” fluffy (gahabok) FOR HYPERTHYROIDISM PROPYLTHIOURACIL (PTU) AND METHIMAZOLE Used to control overactive thyroid due to Graves disease, toxic nodular goiter. Methimazole is 10 times potent than PTU and has a longer half-life and the euthyroid state is achieved in 2 to 4 months. Drug Interactions: o Oral anticoagulants (warfarin) – can cause increase in anticoagulation effect. o Thyroid drugs decreased the effects of insulin and oral antidiabetics. GLUCOCORTICOIDS Nursing Responsibilities: Glucocorticoids are influenced by ACTH, which is o Teach patient to take drug with meals to decrease released from the anterior pituitary gland. gastrointestinal symptoms. o Advise patient about effects of iodine and its They affect carbohydrate, protein, and fat metabolism and presence in iodized salt, shellfish, and OTC cough muscle and blood cell activity. medicines. Because of their many mineralocorticoid effects, o Emphasize importance of drug compliance; abruptly glucocorticoids can cause sodium absorption from the stopping antithyroid drug could bring on thyroid crisis. kidney, resulting in water retention, potassium loss, and o Teach patient signs and symptoms of increased blood pressure. hypothyroidism: lethargy, puffy eyelids and face, thick Cortisol, the main glucocorticoid, has anti-inflammatory, tongue, slow speech with hoarseness, lack of antiallergic, and antistress effects. perspiration, and slow pulse. Hypothyroidism can Indications for glucocorticoid therapy include trauma, result from treatment of hyperthyroidism. surgery, inflammation, emotional upsets, and anxiety. o Advise patient to avoid antithyroid drugs if pregnant Cortisone drugs have several routes of administration: or breastfeeding. Antithyroid drugs taken during oral, parenteral (IM or IV), topical (creams, ointments, lotions), and aerosol (inhaler). Side Effects and Adverse Reactions PATATASLAMANG 3  MODULE 7: ENDOCRINE DRUGS o Increased blood sugar MINERALOCORTICOIDS o Abnormal fat deposits in the face and trunk (so-called Second type of corticosteroid, secrete aldosterone. moon face and buffalo hump) Aldosterone is controlled by the renin angiotensin system, o Decreased extremity size not by ACTH. o Muscle wasting o Edema o Sodium and water retention o Hypertension o Euphoria or psychosis o Thinned skin with purpura o Increased intraocular pressure (glaucoma) o Peptic ulcers o Growth retardation o Long-term use: Adrenal atrophy (loss of adrenal gland function) Nursing Responsibilities: o Determine vital signs. Glucocorticoids such as prednisone can increase blood pressure and sodium and water retention. o Administer glucocorticoids only as ordered. Routes of These hormones maintain fluid balance by promoting the administration include oral, IM (not in deltoid muscle), reabsorption of sodium from the renal tubules. IV, aerosol, and topical. Apply topical glucocorticoids Mineralocorticoid deficiency usually occurs with in thin layers. Rashes, infection, and purpura should glucocorticoid deficiency, frequently called corticosteroid be noted and reported. deficiency. o Record weight. Report weight gain of 5 lb in several Fludrocortisone (Florinef) is an oral mineralocorticoid that days; this would most likely be caused by water can be given with a glucocorticoid. retention. Because potassium excretion occurs with the use of o Monitor laboratory values, especially serum mineralocorticoids and glucocorticoids, the serum electrolytes and blood sugar. Serum potassium level potassium level should be monitored. could decrease to < 3.5 mEq/L, and blood sugar level would probably increase. ANTIDIABETIC DRUGS o Watch carefully for signs and symptoms of These are used primarily to control diabetes mellitus, a hypokalemia: nausea, vomiting, muscular weakness, chronic disease that affects carbohydrate metabolism. abdominal distention, paralytic ileus, and irregular Two groups of antidiabetic agents: heart rate. o Insulin- a protein secreted from the beta cells of the o Assess for side effects from glucocorticoid drugs pancreas, is necessary for carbohydrate metabolism when therapy has lasted more than 10 days and drug and plays an important role in protein and fat is taken in high dosages. Cortisone preparation metabolism. should not be abruptly stopped, because adrenal o Oral hypoglycemic (antidiabetic) drugs- are synthetic crisis can result. preparations that stimulate insulin release or o Monitor older adults for signs and symptoms of otherwise alter the metabolic response to increased osteoporosis. Glucocorticoids promote hyperglycemia calcium loss from bone. Glucagon – alpha cells o Report changes in muscle strength. High doses of glucocorticoids promote loss of muscle tone. Insulin – beta cells Health Teaching: Glucagon increases the sugar in blood o Advise patient to take drug as prescribed. Caution Insulin – decreases the sugar in blood through going inside the cells patient not to abruptly stop drug. When drug is DIABETES discontinued, dose is tapered over 1 to 2 weeks. A chronic disease resulting from deficient glucose o Prepare schedule for patient to decrease dose over 4 metabolism, is caused by insufficient insulin secretion to 5 days. For short-term use ( Baseline Data reduce elevated intraocular pressure; most common o Obtain baseline values for serum potassium, along use of Carbonic anhydrase inhibitors with baseline values for weight, blood pressure o Urinary alkalinization- increasing urinary pH – (sitting and supine), pulse, respiration, sodium, and enhances renal excretion of cystine and other weak chloride. acids- 2-3 d effect o For patients with edema, record sites and extent of o acute mountain sickness – used as prophylaxis - edema rapid ascent above 10,000 ft – given nightly before o Use with caution in patients taking ACE inhibitors, ascent – cerebral and pulmonary edema angiotensin receptor blockers, and direct renin o metabolic alkalosis -alkalosis due to excessive use of inhibitors. diuretics in heart failure o epilepsy – both grand mal & petit mal- reduces LOOP DIURETICS severity & magnitude of seizures- in conjunction with These drugs produce more loss of fluid and electrolytes antiepileptic medications to enhance action than any other diuretics. They are known as loop diuretics ▪ hydrocephalus- reduces the rate of CSF because their site of action is in the loop of Henle. formation and decreases cerebral spinal fluid pH Loop diuretics inhibit the cotransport of Na + /K+ /2Cl− in Pharmacokinetics: the luminal membrane in the ascending limb of the loop of o well absorbed orally or topically for Henle. o glaucoma – applied topically 2-4x daily PATATASLAMANG 2  MODULE 8: RENAL DRUGS Adverse effects: Hypertonic – concentration is higher outside the cell, it will shrink hyperchloremic metabolic acidosis - due to reduction of Hypotonic – pure water no other composition, the cell will swell body bicarbonate stores potassium depletion, drowsiness ELECTROLYTES and paresthesia Preparation SOLUTES o Oral - Acetazolamide(Diamox) tablet 250 mg 1-4x/d Dichlorphenamide 50 mg 1-3x/d; Methazolamide 50- 100 mg 2-3x/d o Topical - Dorzolamide ophthalmic drops 2%, brinzolamide ophthalmic drops DRUGS W/C ALTER EXCRETION OF ORGANIC MOLECULES – URICOSURIC AGENTS Probenecid o Lipid soluble derivative of benzoic acid o Inhibits reabsorption of urate in proximal convoluted tubule – increasing its excretion o Effect on penicillin – inhibits its excretion this increasing plasma concentration o 90% bound to protein o Given orally, well absorbed in GIT, peak concentration – 3h Sulfinpyrazone o Congener of phenylbutazone o Powerful inhibitory effects on uric acid reabsorption in the PCT o Absorbed in GIT o Highly protein bound Indacrinone o Diuretic with uricosuric properties o Main effect of uricosuric drugs: block blood urate reabsorption and lower plasma urate concentration IV FLUIDS P.I.S.O BASIC TYPES OF INTRAVENOUS FLUIDS Potassium – inside (intracellular) Sodium – out (extracellular) SODIUM Sodium - most abundant cation in ECF and a major contributor to serum osmolality. Normal serum sodium levels - 135 to 145 mEq/L Colloids – plasma expanders, adds bulkiness of fluid inside the Sodium is found in many foods: bacon, ham, processed body. You give to maintain oncotic pressure cheese, and table salt Reabsorption o 2/3 Proximal Convoluted Tubule o 25-30% Thick Ascending Loop of Henle o 5-10% Distal Convoluted Tubule HYPONATREMIA Low sodium intake Clinical Features: o Cellular swelling o Primary neurologic: cerebral edema o Early symptoms: nausea, headache and vomiting o Severe complications: seizures, brainstem herniation, normocapneic respiratory failure, coma and death COMPOSITION OF IV FLUIDS HYPERNATREMIA Clinical Features o Cellular shrinkage o Predominantly neurologic o Altered mental status o Vascular complication (pediatric/neonates) o Rhabdomyolysis o Patients with chronic hypernatremia are less likely to Isotonic – cells remain the same develop severe neurologic compromise PATATASLAM