Anti-inflammatory and CNS Drugs - Student Notes

Antiinflammatory Drugs Inflammation & Arachidonic Acid Pathway: Localized protective response: - Stimulated by injury to tissues - which serves to destroy, dilute, or wall off (sequester) both the injurious agent...

Antiinflammatory Drugs Inflammation & Arachidonic Acid Pathway: Localized protective response: - Stimulated by injury to tissues - which serves to destroy, dilute, or wall off (sequester) both the injurious agent and the injured tissue - Want to prevent further damage to other areas - Pain, fever, loss of function, redness, swelling - Endogenous compounds, including proteins of the complement system, histamine, serotonin, bradykinin, leukotrienes, and prostaglandins Leukotriene & Prostaglandin pathways NSAIDs (Nonsteroidal Antiinflammatory Drugs) Indications: Salicylates: Acetic Acid Derivatives: Propionic Acid - Large and chemically diverse group of drugs w/ the following properties: - Analgesic salicylic acid (Aspirin) indomethacin (Indocin) Derivatives: - Anti-inflammatory - Inhibits platelet aggregation - Analgesic, anti-inflammatory, - harsh on stomach - Antipyretic - Antithrombotic effect: used in the tx of MI antirheumatic, and antipyretic properties ibuprofen (Motrin, Advil) - Used for fever reduction, pain, inflammation (mainly inflammation) and other thromboembolic disorders - PO, IV, rectal - Most commonly used NSAID - Relief of: - 325mg or 81mg (low-dose aspirin) are - Dose: - Mild to moderate headaches, Myalgia (muscle pain), Neuralgia (nerve pain), given to prevent platelet clotting Indications: - 1 pill, or 200mg, every 4-6hrs Arthralgia (joint pain) - RA, OA, acute bursitis or tendonitis, as needed for pain - Pain associated w/ arthritic disorders (RA, juvenile arthritis, ankylosing Indications: ankylosing spondylitis, acute gouty arthritis, - can go up to 400mg - should spondylitis, OA) - Headache, neuralgia, myalgia, arthralgia PDA, tx of preterm labor not be taking more than - Alleviation of postoperative pain - Pain syndromes resulting from - promotes closure of PDA 1200mg, or 6 pills, per day) - Tx of gout/hyperuricemia inflammation: arthritis, pleurisy, pericarditis - Systemic lupus erythematosus: ketorolac (Toradol) Indications: Mechanism of Action: antirheumatic effects - Some antiinflammatory activity - Analgesic effects in the - Inhibition of the leukotriene pathway, the prostaglandin pathway, or both - Antipyretic action - Used primarily for powerful analgesic effect management of RA, OA, primary - Blocking the chemical activity of the enzyme COX (-1 & -2) - comparable to those of narcotic drugs dysmenorrhea, gout, dental Mechanism of Action: such as morphine pain,musculoskeletal disorders, Adverse Effects: - Irreversible inhibitor of COX-1 receptors - works really well for bone pain antipyretic actions - GI: dyspepsia, heartburn, epigastric distress, nausea, GI bleeding*, mucosal within the platelets themselves lesions* (erosions or ulcerations) - Reduced formation of thromboxane A2, a Indication: naproxen (Naprosyn, - *misoprostol (Cytotec) can be used to reduce effects substance that normally promotes platelet - Short-term use (up to 5 days) to manage - Renal: reductions in creatinine clearance, acute tubular necrosis w/ renal failure aggregation moderate to severe acute pain Aleve) - Renal Function: - Other NSAIDs lack these antiplatelet - Second most commonly used - Use of NSAIDs can compromise existing renal function effects NSAID Adverse Effects: - Renal toxicity can occur in patients w/ dehydration, heart failure, liver - Somewhat better adverse effect - Renal impairment (long-term use), dysfunction, or use of diuretics or ACE inhibitors Adverse Effects: profile than ibuprofen (fewer edema, GI pain, dyspepsia, nausea - Cardiovascular: noncardiogenic pulmonary edema - Reye syndrome: side effects) - BLACK BOX WARNING: ALL NSAIDs (except aspirin) - Acute and potentially life-threatening - Fewer drug interactions w/ ACE - Increased risk of adverse cardiovascular thrombotic effects, including condition involving progressive inhibitors given for HTN fatal MI and stroke neurologic deficits that can lead to coma Cyclooxygenase-2 (COX-2) - Dose: - Use of other NSAIDs may counteract the cardioprotective effects of and may also involve liver damage Inhibitors: - 1 pill every 8-12hrs as needed aspirin - No aspirin to children: Viral illness for pain & aspirin celecoxib (Celebrex) - can increase up to 2 pills, Contraindications: - Salicylism - Salicylate Toxicity - 1st & only remaining COX-2 inhibitor but no more than 660mg, or - Documented aspirin allergy - NOT receive NSAIDs - Cardiovascular: Increase HR 3 pills, per day - Conditions that place the patient at risk for bleeding: Vitamin K deficiency & - CNS: tinnitus, hearing loss, dimness of Indications: Peptic ulcer disease vision, headache, dizziness, - OA, RA, acute pain symptoms, ankylosing - NSAIDs already have a risk for bleeding mental confusion, drowsiness spondylitis, primary dysmenorrhea - GI: N/V, diarrhea - Little effect on platelet function Interactions: - Metab: sweating, thirst, hyperventilation, - Serious interactions can occur when given w/: hypo/hyperglycemia Adverse Effects: - Anticoagulants - Headache, sinus irritation, diarrhea, fatigue, - Aspirin (other NSAIDs) Nursing Implications/Assessment: dizziness, lower extremity edema, HTN - Corticosteroids and other ulcerogenic drugs - PO (pills [enteric coated, combo products], - Protein bound drugs liquids), topical cream, rectal suppositories Contraindications: - Diuretics and ACE inhibitors - Administered at 1st sign of MI: - DO NOT Use if patient as a known sulfa - prevent clot from forming, prevent allergy Nursing Implications/Assessment: long-term damage from clot - Sulfa antibiotics and Celebrex share a - Perform and assess laboratory studies as indicated (cardiac, renal, and liver - Daily tablet (81mg or 325mg): similar structure function studies; complete blood count; platelet count) prophylactic therapy for adults who - Educate patients about various adverse effects of NSAIDs. Instruct them to have strong risk factors for developing notify their prescribers if these effects become severe or if bleeding or GI pain coronary artery disease or occurs cardiovascular accident Enolic Acid Derivatives: - 81- and 325-mg strengths appear to - better tolerated gastrointestinally than some - Instruct patients to watch closely for the occurrence of any unusual bleeding, be equally beneficial for the other NSAIDs such as in the stool - Monitor for therapeutic effects, which vary according to the condition being tx prevention of thrombotic events Indications: - Decrease in swelling, pain, stiffness, and tenderness of a joint or muscle area - Tx mild to moderate OA, RA, gouty arthritis Antigout Drugs: Herbal Products: Gout/Hyperuricemia: Glucosamine & Chondroitin - Condition that results from inappropriate uric acid metabolism - Used to tx pain of OA - Underexcretion of uric acid - Overproduction of uric acid Adverse Effects: - Uric acid crystals are deposited in tissues and joints, resulting in pain - GI discomfort - Drowsiness, headache, skin reactions (glucosamine) Goal of Tx: - Decrease the symptoms of an acute attack and prevent recurrent attacks Interactions: - Enhances effects of warfarin (increases bleeding) 1st-line Therapy: - May increase insulin resistance (glucosamine) - NSAIDs 2nd-line Therapy: allopurinol (Zyloprim) - Used to prevent uric acid production and to prevent acute tumor lysis syndrome Adverse Effects: - Exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis  Analgesics Analgesics: Opioids - Medications that relieve pain w/o causing loss of consciousness - “Painkillers” - Synthetic drugs that bind to the opiate receptors to relieve pain Adverse Effects: Contraindications: - Opioid Analgesics - Mild agonists: - CNS depression - Known Drug Allergy - Adjuvant analgesic drugs - Codeine, hydrocodone - leads to resp depression (most serious adverse effect) - Severe asthma - Strong agonists: - N/V - Use w/ extreme caution in patients w/: Pain: - Morphine, hydromorphone, oxycodone, oxymorphone, - Stimulate chemoreceptor trigger zone in CNS - Administer - Respiratory insufficiency - An unpleasant sensory and emotional experience meperidine, fentanyl, methadone w/ food - Elevated intracranial pressure associated w/ actual or potential tissue damage - A personal and individual experience - Meperidine: - Urinary retention - Morbid obesity or sleep apnea - Not recommended for long-term use b/c of the - Diaphoresis and flushing - Paralytic ileus - Whatever the patient says it is - Pupil constriction (miosis) - opioids already cause constipation - don’t want to accumulation of a neurotoxic metabolite, - Exists when the patient says it exists - Constipation - slow peristalsis make bowel function worse normeperidine, which can cause seizures - Opiate Ceiling Effect: - Administer laxative when patient ordered for opioids - Pregnancy - Drug reaches a maximum analgesic effect - Itching - Can cross placenta to fetus WHO Three-Step Analgesic Ladder: - Analgesia does not improve, when with higher doses - Switch opioids or give Benadryl Interactions: Step 1: Indications: - Tolerance: - Alcohol, antihistamines, barbiturates, benzodiazepines, - Nonopioids (w/ or w/o adjuvant meds) - Main use: - Common physiologic result of chronic opioid tx MAOIs, other CNS depressants - After pain assessed and identified - To alleviate moderate to severe pain - Result: larger dose is required to maintain the same - If pain persists or increases, tx moves to: level of analgesia Nursing Implications/Assessment: - Administered w/ adjuvant analgesic: Step 2: - Physical Dependence: - Equianalgesia - Assist primary drugs (opioids) w/ pain relief - Opioids w/ or w/o nonopioids and w/ or w/o adjuvants - Physiologic adaptation of the body to the presence of an - Ability to provide equivalent pain relief by calculating - Also used for: - If pain persists or increases, management then rises to: opioid dosages of different drugs or routes of administration - Cough center suppression - Will need to be weaned off med, may need tx to get off that provide comparable analgesia Step 3: - Tx of diarrhea - Hydromorphone (Dilaudid): Seven times more potent - Opioids indicated for moderate to severe pain - Balanced anesthesia med - Can die from stopping cold turkey than morphine - Administered w/ or w/o nonopioids or adjuvant - Not for Chronic Pain Tx - Psychological Dependence - Addiction - Ex. morphine 10mg + hydromorphone 1mg (one hour medications - Tx Acute Pain - A pattern of compulsive drug use characterized by a later) = 17mg morphine - Pain that normally fades w/ healing, is r/t tissue damage and continued craving for an opioid and the need to use the - Risk for drug toxicity and overdose significantly alters a patient’s typical function, and is expected opioid for effects other than pain relief - Opioid Naive: Adjuvants: to be time-limited - Someone who has never been on opioids before - do - Assist primary drugs in relieving pain Mechanism of Action: Toxicity/Overdose: not want to give full dose (want to give 1/2 at first and - NSAIDs - Agonists: - Opioid Antagonists: increase from there) - Antidepressants - Bind to an opioid pain receptor in the brain - Naloxone (Narcan) - Morphine Equivalent Daily Dose (MED): - Anticonvulsants - Cause an analgesic response (reduction or pain sensation) - Naltrexone (ReVia) - Conversion of various opioid analgesics to a morphine - Corticosteroids - Agonists-antagonists: - Uses: Tx of opioid overdose and toxicity equivalent dose by the use of accepted conversion - Ex. adjuvant drugs for neuropathic pain - Bind to a pain receptor - Will remove all opioid in system tables provided by the state board of pharmacy - Amitriptyline (antidepressant) - Cause a weaker neurologic response than a full agonist - Administered for severe resp depression - The total morphine equivalent dose (MED) may not - Gabapentin or pregabalin (anticonvulsants) - Also called partial agonist or mixed agonist - Regardless of withdrawal S/Sx exceed an average of 30 MED per day except - Antagonists (non-analgesic): - Opioid withdrawal (abstinence syndrome): - Tx patients who suffer from medical conditions, surgical - Reverse the effects of these drugs on pain receptors - Anxiety, irritability, chills and hot flashes, joint pain, outcomes, or injuries of such severity that pain cannot lacrimation, rhinorrhea, diaphoresis, N/V, abdominal be managed within 30 MED average limit as determined Scheduled Drugs: - Bind to a pain receptor and exert no response - Also known as competitive agonists cramps, diarrhea, constipation by the treating physician based upon prevailing Schedule I: standards of medical care, such as: - No currently accepted medical use and a high potential - Traumatic crushing of tissue for abuse - Ex. heroin, LSD, marijuana, ecstasy, methaqualone, Methadone hydrochloride (Dolophine) - Amputation - Synthetic opioid analgesic (Schedule II) - Major orthopedic surgery peyote - Severe burns - Opioid of choice - Detoxification tx of opioid addicts - Cancer Schedule II: Codeine Sulfate - Methadone maintenance programs - Drugs w/ a high potential for abuse, w/ use potentially - Used to tx chronic (e.g., neuropathic) and cancer-related - Natural opiate alkaloid (Schedule II) obtained from opium pain leading to severe psychological or physical dependence - Similar to morphine in terms of its pharmacokinetic and - Prolonged half-life of the drug: Cause of unintentional - Ex. combo products w/ less than 15mg of hydrocodone pharmacodynamic properties overdoses and deaths per dosage unit (Vicodin), cocaine, methamphetamine, - 10% of codeine is metabolized to morphine - Cardiac dysrhythmias methadone, hydromorphone (Dilaudid), meperidine - For mild-to-moderate pain (Demerol), oxycodone (OxyContin), fentanyl, Dexedrine, Adderall, Ritalin - Less effective Morphine Sulfate - Ceiling effect - only agonist - Naturally occurring alkaloid derived from the opium poppy Naloxone hydrochloride (Narcan) 1. Has a high potential for abuse - More commonly used as an antitussive drug - Pure opioid antagonist - Prototype opioid drug: Schedule II controlled substance 2. Has currently accepted medical use in tx in the USA or a - GI disturbance - give w/ food to minimize - Drug of choice for the complete or partial reversal of - Indication: Severe pain currently accepted medical use w/ severe restrictions - No longer used in pediatric patients opioid-induced respiratory depression - High abuse potential 3. May lead to severe psychological or physical dependence - Risk for deaths due to CYP450 metab issues - Indication: - PO, injectible (PCA), and rectal dosage forms; also if abused - Suspected acute opioid overdose - drug overdose extended-release forms - Ex. hydrocodone, oxycodone, morphine, Fentanyl - Never crush extended-release morphine (MS Contin) - will methamphetamine - Synthetic opioid (Schedule II) - Tx moderate-to-severe pain - IV, transdermal patches, buccal lozenges, buccal lozenges on a overdose Buprenorphine w/ naloxone Schedule III: stick Oxycodone hydrochloride (Suboxone) - Drugs w/ a moderate to low potential for physical and - Fentanyl patches - only for chronic or cancer pain - Analgesic drug - comparable to morphine (Schedule II) - Partial agonists w/ opioid antagonists (Schedule III) - 4 to 1 psychological dependence - Fentanyl - 0.1mg VI = 10mg morphine IV - Commonly combined in tablet form w/ acetaminophen ratio - Ex. combo products w/ less than 90mg of codeine per - Highly effective in tx cancer pain (Percocet) and w/ aspirin (Perdocan) - Detoxification tx of opioid addicts dosage unit (Tylenol w/ codeine), ketamine, anabolic - Do not sue for opioid naive patients - Immediate release (Oxy IR) and sustained-release formulas - Side Effects: steroids, testosterone (Oxycontin) - Headache, diarrhea, constipation, nausea Hydromorphone (Dilaudid) - Hydrocodone - weaker by commonly used opioid - Similar side effects as opioids Schedule IV: - Very potent opioid analgesic; Schedule II drug - Drugs w/ a low potential for abuse and low risk of - Only available in tablet form - 1mg of IV or IM = 7mg morphine - Commonly combined w/ acetaminophen (Vicodin and dependence - Ex. Xanax, Soma, Darvon, Darvocet, Valium, Ativan, Norco) Talwin, Ambien, Tramadol - Schedule II drug Schedule V: - Drugs w/ lower potential for abuse than Schedule IV and consist of preparations containing limited quantities of Nonopioid Analgesics certain narcotics - Generally used for antidiarrheal, antitussive, and analgesic purposes Acetaminophen (Tylenol) Tramadol hydrochloride (Ultram) - Ex. cough preparations w/ less than 200mg of codeine - Analgesic and antipyretic effects - Centrally acting analgesic w/ a dual mechanism of action or per 100mL (Robitussin AC), Lomotil, Motofen, Lyrica, Dosage: - No anti-inflammatory - Maximum daily dose for healthy adults is 3000mg/day - Weak bond w/ opioid receptors and inhibits the reuptake Parepectolin - Available OTC, in combo w/ opioids of both NE and serotonin - 2000mg for older adults and those w/ liver disease - Inadvertent excessive doses may occur when different - Tx of moderate to moderately severe pain (not classified Indications: combination drug products are taken together as an opioid) Nursing Implications/Assessment: - Mild to moderate pain - Be aware of the acetaminophen content of all medications - Interactions (Result in seizures): - Perform a thorough pain assessment - Fever take by the patient (OTC and prescription) - Tricyclic antidepressants, selective serotonin reuptake - “Fifth vital sign” - Alternative for those who cannot take aspirin products inhibitors (SSRIs), monoamine oxidase inhibitors - Rate pain on a 0 to 10 or similar scale (MAOIs), neuroleptics - Pain management includes pharmacologic and Toxicity and Managing Overdose: Mechanism of Action: - Even though available OTC, lethal when overdosed - cannot give w/ antidepressants nonpharmacologic approaches - Be sure to include nonpharmacologic approaches as - Similar to salicylates - Overdose - Causes hepatic necrosis: hepatotoxicity indicated - Blocks pain impulses peripherally by inhibiting prostaglandin - Hepatotoxicity - Can also be caused by long-term - Oral forms of opioids: synthesis ingestion of large doses Feverfew - Herbal Product - Take w/ food to minimize GI upset - Recommended antidote: acetylcysteine regimen - R/t the marigold family - Common adverse effect: Constipation Interactions: - Anti-Inflammatory properties - Prevent is the key - adequate fluid and fiber intake - Should not be taken in the presence of: - Used to tx migraine headaches, menstrual cramps, - Monitor for adverse effects - Drug allergy inflammation, and fever - Contact physician immediately if vital signs change, a - Liver dysfunction - May cause GI distress, altered taste, muscle stiffness patient’s condition declines, or pain continues - Possible liver failure - May interact w/ aspirin and other NSAIDs, as well as - Respiratory depression: - G6PD deficiency anticoagulants - Less than 10 breaths/min, dyspnea, diminished - Dangerous interactions may occur if taken w/ alcohol or other breath sounds, shallow breathing drugs that are hepatotoxic - Monitor for therapeutic effects: - Decreased complains of pain, decreased severity of pain, increased periods of comfort, decreased fever (acetaminophen) - Improved ADLs, appetite, and sense of wellbeing  CNS Depressants + Muscle Relaxants Sedatives: Benzodiazepines Barbiturates - Drugs that have an inhibitory effect on the CNS to the degree that they reduce: - Nervousness - Previously most commonly prescribed sedative-hypnotic drugs - 1st introduced in 1903; were the standard drugs for - Excitability - Currently nonbenzodiazepines are more frequently prescribed insomnia and sedation - Irritability - Favorable drug effect profiles, efficacy, and safety - Habit forming; low therapeutic index - Classified as either: - Only a handful commonly used today - Sedative-hypnotic - Due to the safety and efficacy of Hypnotics: - Anxiolytic (med that relieves anxiety) benzodiazepines - Cause sleep - Much more potent effect on CNS than Indications: Four Categories: sedatives - Sedation - Ultrashort acting: - A sedative can become a hypnotic if - Sleep induction - Anesthesia for short surgical procedures, other uses given in large enough doses - Skeletal muscle relaxation - Short acting: - Anxiety relief - Sedation and control of convulsive conditions Nursing Implications/Assessment: - Anxiety-related depression - Intermediate acting: - Rebound insomnia - may occur a few nights - Tx of acute seizure disorders - Sedation and control of convulsive conditions after a 3-4 week regimen has been - Tx of alcohol withdrawal - Long acting: discontinued - Agitation relief - Sleep induction, epileptic seizure prophylaxis - Safety is important: - Balanced anesthesia - Keep side rails up or use bed alarms - Moderate or conscious sedation Indications: - Do not permit smoking - Tx of muscle spasms/spasticity - Sedatives - Assist patient w/ ambulation (especially - Anticonvulsants older adults) Mechanism of Action: - Anesthesia for surgical procedures - Keep call light within reach - Depress CNS activity - Monitor for adverse effects - Affect hypothalamic, thalamic, and limbic systems of the brain Mechanism of Action: - Benzodiazepine receptors (in the brain) - Site of Action: brainstem (reticular formation) Therapeutic Effects: - Gamma-aminobutyric acid (GABA) - Potentiates the action of GABA - inhibits the nerve - Increased ability to sleep at night - Do not suppress rapid eye movement (REM) sleep as much as barbiturates do impulses that are traveling in the cerebral cortex - Fewer awakenings - Do not increase metab of other drugs - Shorter sleep-induction time Adverse Effects: - Few adverse effects, such as “hangover” Adverse Effects: - Drowsiness, lethargy, Dizziness, hangover, paradoxical effects - Mild and Infrequent: restlessness or excitement - Improved sense of well-being b/c of - Headache, drowsiness, dizziness, cognitive impairment, vertigo, lethargy, fall hazard for older adults, - Reduced REM sleep, resulting in: improved sleep “Hangover” effect or daytime sleepiness - Agitation, inability to deal w/ normal stress: - For muscle relaxants: decreased spasticity, decreased rigidity Interactions: Interactions: - Overall, decreased pain - Azole antifungals, verapamil, diltiazem, protease inhibitors, macrolide antibiotics, grapefruit juice - Additive effects: - CNS depressants (alcohol, opioids) - Alcohol, antihistamines, benzodiazepines, opioids, - Olanzapine Muscle Relaxants - Rifampin tranquilizers - Inhibited metabolism - MAOIs prolong the effects of barbiturates - Relieve pain associated w/ skeletal muscle Therapeutic Effects: - Increased metabolism spasms - Calming effect on the CNS - Reduces anticoagulant response, leading to - Majority are centrally acting - Useful in controlling agitation and anxiety possible clot formation - CNS is the site of action - Reduce excessive sensory stimulation, inducing sleep - Similar in structure and action to other - Induce skeletal muscle relaxation Therapeutic Effects: CNS depressants - Low doses: sedative effects - Direct acting Long-Acting: - High doses: hypnotic effects (also lower resp rate) - Act directly on skeletal muscle - Notorious enzyme inducers - Closely resemble GABA diazepam (Valium) - Stimulate liver enzymes that cause metab or - Benzodiazepines can be used as muscle - 1st clinically available benzodiazepine drug breakdown of many drugs relaxants - Uses: - Result in shortened duration of action - Anxiety Indications: - Procedural sedation and anesthesia adjunct - Relief of painful musculoskeletal conditions - Anticonvulsant therapy Phenobarbital - Skeletal muscle relaxant - Prototypical barbiturate - Muscle spasms - Management of spasticity of severe - Long-acting drug chronic disorders (multiple sclerosis, Short-Acting: - Uses: cerebral palsy) midazolam (Versed) - Prevention of generalized tonic-clonic seizures - Work best when used along w/ physical and fever-induced convulsions, as well as tx of - Most commonly used preoperatively and for moderate sedation therapy hyperbilirubinemia in neonates - Causes amnesia and anxiolysis (reduced anxiety) as well as sedation - want to do something to help strengthen - Rarely used today as a sedative - IV or PO muscles and prevent muscle spasms - No longer recommended to be used as a hypnotic from occurring drug Nonbenzodiazepines Adverse Effects: Short-Acting: - Extension of effects on CNS and skeletal OTC Hypnotics muscles: eszopiclone (Lunesta) - 1st hypnotic to be FDA approved for long-term use - Euphoria, lightheadedness, dizziness, - Designed to provide a full 8hrs of sleep - Nonprescription sleeping aids often contain drowsiness, fatigue, muscle weakness, - Considered a short- to intermediate-acting agent antihistamines, which have CNS depressant effects others - Patients should allot 8hrs of sleep time - Concurrent use w/ alcohol - causes respiratory - Avoid taking hypnotics if not able to dedicate 8hrs to sleep (minimum 6hrs) depression or arrest Methocarbamol (Robaxin) - As will all CNS depressants zolpidem (Ambien) - Short-acting nonbenzodiazepine hypnotic - Lower incidence of daytime sleepiness compared with benzodiazepine hypnotics - Ambien CR is a longer acting form w/ two separate drug reservoirs - Somnambulation (sleep walking)  CNS Stimulants - Drugs that stimulate a specific area of the brain or spinal cord Therapeutic Effects: - Sympathomimetic drug ADHD: - Classified 3 ways according to: - Decreased hyperactivity, increased attention span and concentration - Chemical structure: - Amphetamines, serotonin antagonists, sympathomimetics, xanthines Narcolepsy: - Site of action in the CNS - Decrease in sleepiness - Therapeutic Use: anti-attention deficit disorder, anti-narcoleptic, anorexiant, antimigraine, analeptic drugs Anorexiant: - Appetite control and weight loss Serotonin agonist (SSRAs): - Decrease in frequency, duration, and severity of migraines Principle Drugs Used to Tx ADHD and Narcolepsy: Anorexiants: Antimigraine Drugs: Amphetamines: - Used to tx obesity Selective Serotonin Receptor Mechanism of Action: Mechanism of Action: Agonists (SSRAs) - end in - Stimulate areas of the brain associated w/ mental alertness - Suppress appetite control centers in the brain “-triptan” - Increase the body’s basal metabolic rate Adverse Effects: Mechanism of Action: - Mobilization of adipose tissue stores - Wide range; dose related - Stimulate 5-HT receptors in cerebral arteries, - Enhanced cellular glucose uptake - Tend to “speed up” body systems causing vasoconstriction and reducing headache - Reduce dietary fat absorption - Addictive properties symptoms - Palpitations, tachycardia, HTN, angina, dysrhythmias, nervousness, restlessness, anxiety, insomnia, - Reduce the production of inflammatory Adverse Effects: neuropeptides N/V, diarrhea, dry mouth, increased urinary frequency - Possible elevated BP, heart palpitations, anxiety, agitation, dizziness, headache Therapeutic Effects: Adverse Effects: - CNS effects: - Vasoconstriction Nursing Implications/Assessment: - Irritation at injection site - Mood elevation or euphoria - Follow instructions for diet and exercise - Tingling, flushing - Increased mental alertness and capacity for work - Take in the morning - Decreased fatigue and drowsiness - Avoid caffeine - Prolonged wakefulness Nursing Implications/Assessment: - Do not want to take 2 CNS stimulants - Respiratory effects: - Dissolvable wafers, nasal spray, - Fat-soluble vitamin supplementation may be needed - Relaxation of bronchial smooth muscle self-injectable forms - Increased respiration - Provide specific teaching about correct - Dilation of pulmonary arteries Orlistat (Xenical) administration - Related non-stimulant drug used to tx obesity - Instruct patients to keep a journal to monitor Nursing Implications/Assessment: response to therapy - Last daily dose should be given 4-6hrs before bedtime to reduce insomnia Mechanism of Action: - Take on an empty stomach 30-45min before meals - Works locally in the small and large intestines, where it Sumatriptan (Imitrex) - Drug “holidays” may be ordered inhibits absorption of caloric intake from fatty - original prototype drug - Instruct patients to keep a journal to monitor the child’s response to therapy foods - Monitor the child for continued physical growth, including height and weight - Binds to gastric and pancreatic enzymes called - Potential for weight loss lipases Non-amphetamine Stimulants: Adverse Effects: Atomoxetine (Strattera) - Oily spotting, flatulence, fecal incontinence in 20-40% of patients - Non-stimulant drug also used for ADHD - Approved for tx ADHD in children older than 6 years of age and in adults - Lacks addictive properties - Sept. 2005 - FDA Warning - Suicidal thinking and behavior in small numbers of adolescent patients Analeptics: receiving this medication - Stimulate areas of CNS that control respiration - Used for neonatal apnea Methylphenidate (Ritalin) Methylxanthines (theophylline) - 1st prescription drug indicated for ADHD - Also used for narcolepsy - Inhibit phosphodiesterase, leading to buildup of cyclic adenosine monophosphate (cAMP) - Extended-release dosage forms - Relaxes smooth muscle in the respiratory tract Modafinil (Provigil) Caffeine - Use: Improvement of wakefulness in patients w/ excessive daytime sleepiness (narcolepsy) and shift - Antagonizes adenosine receptors work sleep disorder - Associated w/ sleep promotion - Less abuse potential than amphetamines and methylphenidate - Found in: - Schedule IV drug - OTC: NoDoz - Combo prescription drugs - Food and beverages - Use w/ caution in patients w/ a history of: - Peptic ulcer - Recent myocardial infarction - Dysrhythmias - Intravenous: - Caffeine citrate (neonatal apnea) and caffeine sodium benzoate (respiratory depression in adults)  Antiepileptic Drugs (AEDs) - AKA anticonvulsants Barbiturates: Gabapentin (Neurotin) - Goals of Therapy: Phenobarbital & Primidone (Myosline) - Chemical analogue of GABA, a - To control or prevent seizures while maintaining a reasonable quality of life neurotransmitter that inhibits brain activity - To minimize adverse effects and drug-induced toxicity - Primidone is a prodrug that is metabolized in the liver into - AED therapy is usually lifelong phenobarbital - Combo of drugs may be used - Lower serum level than phenobarbital - decreases level of Indication: - Single-drug therapy is started before multiple-drug therapy is tried sedation - Partial seizures - Serum drug concentrations must be measured - Most common adverse effect: sedation - Effective single-drug therapy for new - Therapeutic drug monitoring - Will develop tolerance over time onset epilepsy - Serum concentrations of phenytoin, phenobarbital, carbamazepine, and primidone correlate better - Neuropathic pain (diabetics) w/ seizure control and toxicity than do those of valproic acid, ethosuximide, and clonazepam Adverse Effects: - Antiepileptic drugs traditionally used to manage seizure disorders include: - CV, CNS, GI, and dermatologic reactions Mechanism of Action: - Barbiturates, Hydantoins, Iminostilbenes plus valproic acid, and 2nd- and 3rd-gen AEDs - Believed to work by increasing the Contraindications: synthesis and synaptic accumulation of Indications: - Known drug allergy, porphyria, liver or kidney impairment, and GABA between neurons - Prevention or control of seizure activity resp illness - Long-term maintenance therapy for chronic, recurring seizures Adverse Effects: - Acute tx of convulsions and status epilepticus Interactions: - CNS and GI symptoms - Alters the CYP450 enzyme metab - reduced effect of multiple Mechanism of Action: drugs - exact mechanism of action is unknown Pregabalin (Lyrica) - Schedule V controlled substance Adverse Effects: Hydantoins: - Structurally related to GABA - Numerous; vary per drug - Adverse effects often necessitate a change in medication Phenytoin (Dilantin) Indication: - Black Box Warning as of 2008 - has been used as a 1st-line drug for many years and is the - Adjunct therapy for partial seizures - Suicidal thoughts and behavior prototypical drug - Neuropathic pain, postherpetic neuralgia, - Mental status changes, mood changes, changes in LOC or sensorium fibromyalgia - Suicidal thoughts or ideas Adverse Effects: - Eye problems, visual disorders - Lethargy, abnormal movements, mental confusion, cognitive Adverse Effects: - Sore throat, fever (blood dyscrasias may occur w/ hydantoins) changes - Primarily CNS related - Drowsiness, many others - Gingival hyperplasia, acne hirsutism, Dilantin facies, osteoporosis Contraindications: - Known Drug Allergy Contraindication: - Pregnancy - usually still given - Heart conditions that involve bradycardia - Risk vs Benefit: major seizures will kill both mom and fetus Nursing Implications/Assessment: Therapeutic Effects: - IV administration - Reduce nerve’s ability to be stimulated - Very irritating to veins - Suppress transmission of impulses from one nerve to the next - Slow IV directly into a large vein through a large-gauge - Decrease speed of nerve impulse conduction within a neuron (20-gauge or larger) venous catheter - Decreased or absent seizure activity - Diluted in normal saline (NS) for IV infusion - Infiltration from IV will cause necrosis to surrounding tissues Nursing Implications/Assessment: - Oral Drugs: - Take regularly, same time each day Carbamazepine (Tegretol) - Take w/ meals to reduce GI upset - 2nd most commonly prescribed antiepileptic in US after - Do not crush, chew, or open extended-release forms phenytoin - If patient is NPO for a procedure, contract prescriber regarding AED dosage - Autoinduction of hepatic enzymes - creates enzymes that - Teach patients to keep a journal to monitor: metabolize the drug - Response to AED - Results in decreased levels - Seizure occurrence and descriptions - Adverse Effects & Drug Interactions are numerous - Adverse effects - Instruct patients to wear a medical alert tag or ID - AEDs should not be discontinued abruptly Indications: - Teach patients that therapy is long-term and possibly lifelong (not a cure) - Partial seizures and generalized tonic-clonic seizures - Teach patients that, to prevent complications, they should call the healthcare provider if they experience fever, sore throat, excessive bleeding or bruising and new onset of nosebleeds Contraindicated: - Myoclonic and absence seizures  Antiparkinson Drugs Parkinson’s Disease: Nursing Implications/Assessment: - Chronic, progressive, degenerative disorder - When starting dopaminergic drugs, assist patient w/ walking b/c dizziness may occur - Affects dopamine-producing neurons in the brain - Administer oral doses w/ food to minimize GI upset - Caused by an imbalance of Dopamine and Ach - Encourage patient to force fluids to at least 3000mL/day (unless contraindicated) - **Dopamine - lack of; majorly stems from not enough dopamine - Taking levodopa w/ MAOIs may result in HTN crisis - Acetylcholine (ACh) - increase of - Teach patient: - Classic Symptoms: - Do not discontinue antiparkinson drugs suddenly - Akinesia (inability to control movements of muscles) - Expected therapeutic and adverse effects w/ antiparkinson drug therapy - Bradykinesia (slowing of movements) - Monitor for response to drug therapy: - Postural instability (b/c muscles aren’t working well anymore) - Improved sense of well-being and mental status - Rigidity, tremor, staggering gait, drooling - Increased appetite - PD is thought to be caused by an imbalance of dopamine and ACh, w/ a deficiency of dopamine - Increased ability to perform ADLs, to concentrate, and to think clearly in certain areas of the brain - Less intense parkinsonian manifestations, such as less tremor, shuffling gait, muscle rigidity, and involuntary - Drug therapies are aimed at increased the levels of dopamine or antagonizing the effects of ACh movements - Unfortunately, current drug therapy does not slow the progression of the disease but rather is - Alcohol, OTC drugs, and herbals are to be avoided unless approved by the prescriber used to slow the progression of symptoms - Six Classes of Medications: MOIs, Dopamine Modulator, Catechol ortho-methyltransferase inhibitors, Nondopamine dopamine receptor agonists, Dopamine replacement drugs, Anticholinergic drugs Dopamine Replacement Drugs: Selective Monoamine Oxidase Dopamine Modulator Anticholinergic Therapy - Replacement drugs (presynaptic) Inhibitors (MAOI) Therapy Amantadine (Symmetrel) - Anticholinergics block the effects of ACh - Used to tx muscle tremors and muscle - MAOs break down catecholamines in CNS, - Antiviral drug used for tx of influenza Levodopa Therapy: rigidity associated w/ PD primarily in the brain - Mechanism of Action: Indirect-acting - These two symptoms are caused by - Levodopa: Biologic precursor of dopamine required by the brain for - Causes release of dopamine and excessive cholinergic activity dopamine synthesis Selective MAO-B Inhibitors: other catecholamines from their - Does not relieve bradykinesia (extremely - Work presynaptically to increase brain levels of dopamine storage sites - Cause an increase in levels of dopaminergic slow movements) - Levodopa is able to cross the blood-brain barrier, and then it is - In the presynaptic fibers of nerve cells stimulation in CNS - May take several days to a week for converted to dopamine within the basal ganglia - that have - Prevent breakdown of catecholamines beneficial effects of med to be evident - Large doses of levodopa needed to get dopamine to the brain - not yet been destroyed by the disease - dopamine - When used for tx of PD, these meds should Causes adverse effects process - Do not elicit the “cheese effect” of not be take at the same time as other meds - Carbidopa is given w/ levodopa - Blocks the reuptake of dopamine into the nonselective MAOIs used to tx - Should be taken at bedtime - Carbidopa does not cross the blood-brain barrier and prevents nerve fibers depression (if 10mg or less is used) levodopa breakdown in the periphery - Result: Higher levels of dopamine in the - Tyramine containing foods (cheese, Adverse Effects: - As result, more levodopa crosses the blood-brain barrier, where it synapses between nerves and improved red wine, beer, yogurt) - Causes - dry mouth/decreased salivation, urinary can be converted to dopamine dopamine neurotransmission between severe HTN when taken w/ retention, decreased GI motility neurons non-selective MAOIs (constipation), dilated pupils (mydriasis), Mechanism of Action: - Used early in the course of the disease - - Used as monotherapy or as adjuncts w/ and smooth muscle relaxation - Levodopa is taken up by the dopaminergic terminal, converted into Usually effective for only 6-12mo levodopa dopamine, and then released as needed - Used to tx dyskinesia associated w/ - Containdiations: Known drug allergy, - As a result, neurotransmitter imbalance is controlled in patients w/ concurrent sued w/ meperidine carbidopa-levodopa - helps to control Benztropine (Cogentin) early PD who still have functioning nerve terminals tremors, including muscle rigidity - Used for PD and EPS from antipsychotic - Adverse Effects: Increase w/ higher than - Common adverse effects: Dizziness, drugs recommended doses Adverse Effects: insomnia, nausea - Avoid alcohol - Confusion, involuntary movements, GI distress, HoTN, cardiac - Interactions: Increased anticholinergic dysrhythmias adverse effects when given w/ Adverse Effects: anticholinergic drugs - Hyperthermia: Use w/ caution during hot - As PD progresses, it becomes more difficult to control w/ levodopa weather and exercise - Ultimately, levodopa no longer controls the PD, and the patient is - Tachycardia, confusion, disorientation, toxic seriously debilitated Catechol Direct-Acting Dopamine psychosis, urinary retention, dry throat, - This generally occurs between 5-10yrs after the start of Ortho-Methyltransferase Receptor Agonists constipation, N/V levodopa therapy - Non-dopamine dopamine receptor agonists - Anticholinergic syndrome (COMT) Inhibitors (NDDRAs) Carbidopa-Levodopa (Sinemet) Mechanism of Action: - Ergot and Non-ergot derivatives - Block COMT, the enzyme that catalyzes - All of the NDDRAs work by direct - Most commonly used drugs to tx PD the breakdown of the body’s stimulation of presynaptic and/or - Sinemet CR: increases “on” time and decreases “off” time catecholamines postsynaptic dopamine receptors in the - Ability of the drug to tx PD S/Sx - Prolong the duration of action of levodopa; brain - Contraindication: angle-closure glaucoma reduce wearing off phenomenon - Adverse Effects: cardiac dysrhythmias, HoTN, chorea, muscle cramps, GI distress - Interactions: Tricyclic antidepressants, other drugs Adverse Effects: - Best taken on an empty stomach; to minimize GI side effects, it can be - GI upset; urine discoloration; can worsen taken w/ food dyskinesia that may already be present - Tolcapone has been associated w/ cases of severe liver failure Nursing Implications/Assessment: - Assess patient for dizziness and syncope when walking - Administer in the evenings - Meds typically taken w/ food to decrease GI upset - Never omit protein from patient diet - muscles (when is the issue in PD) are all protein  Psychotherapeutic Drugs - Used for tx of emotional and mental disorders Mood-Stabilizing Drugs Antidepressant Drugs - ability to cope w/ emotions can range from occasional depression or anxiety to constant emotional distress - Lithium carbonate and lithium citrate Nursing Implications/Assessment: - When emotions significantly affect an - Other drugs may be used in combo w/ lithium: - Monitor for therapeutic effects: individual’s ability to carry out normal daily - Benzodiazepines, Antipsychotics, - Improved sleep patterns and nutrition, Increased feelings of self-esteem, Decreased feelings of functions, tx w/ a psychotherapeutic drug is a Antiepileptics, Dopamine receptor agonists hopelessness, Increased interest in self and appearance, Increased interest in daily activities, Fewer possible option depressive manifestations or suicidal thoughts or ideations - 3 man emotional and mental disorders: Lithium - Anxiety - Drug of choice for tx of mania - Affective disorders - It is thought to potentiate serotonergic Tricyclic antidepressants: - Psychoses neurotransmission - Have largely been replaced by SSRIs as 1st-line antidepressant drugs - All psychotherapeutic drugs have risk for - Narrow therapeutic range: - Considered 2nd line: suicidal thoughts and harm - High levels produce toxicity: GI discomfort, - For patients who fail w/ SSRIs or other newer generation antidepressants tremor, confusion, somnolence, seizures, and - As adjunct therapy w/ newer generation antidepressants possibly death Indications: Anxiolytic Drugs - Keeping the sodium level in the normal - Depression, childhood enuresis (imipramine), OCDs (clomipramine), adjunctive analgesics for chronic pain range (135-145mEq/L) helps to maintain therapeutic lithium levels conditions such as trigeminal neuralgia Indications: Adverse Effects: Mechanism of Action: - Ethanol withdrawal, insomnia, muscle spasms, - Most serious adverse effect is cardiac - Block reuptake of neurotransmitters, causing accumulation at the nerve endings seizure disorders, adjuncts to anesthesia, dysrhythmias - It is thought that increasing concentrations of neurotransmitters will correct the abnormally low levels that adjunct for depression (anxiety and depression - Drowsiness, slurred speech, epilepsy-type lead to depression occur together) seizures, choreoathetotic movements (involuntary Adverse Effects: Mechanism of Action: wavelike movements of the extremities), ataxia - Sedation, Impotence, ortho HoTN - Reduce anxiety by reducing overactivity in CNS (generalized disturbance of muscular - Older patients: dizziness, postural HoTN, constipation, delayed micturition, edema, muscle tremors coordination), HoTN Nursing Implications/Assessment: - Long-term tx may cause hypothyroidism Overdose: - Monitor for therapeutic effects: - Lethal: 70-80% die before reaching hospital - Improved mental alertness, cognition, and - CNS and CV systems are mainly affected mood Antipsychotic Drugs - Death results from seizures or dysrhythmias - Fewer anxiety and panic attacks - No specific antidote - Improved sleep patterns and appetite - Decrease drug absorption w/ activated charcoal - Less tension and irritability; fewer feelings of - Drugs used to tx serious mental illness - Speed elimination by alkalizing urine fear, impending doom, and stress - Drug-induced psychoses, schizophrenia, - Manage seizures and dysrhythmias - More interest in self and others autism - Provide basic life support - Tx extreme mania (as an adjunct to lithium), BPD, depression that is resistant to other Amitriptyline (Elavil) Benzodiazepines: therapy, certain movement disorders (e.g., - Oldest and most widely used of all the TCAs - Depress activity in the brainstem and limbic Tourette’s syndrome), certain other medical - Original indication was depression system conditions (e.g., nausea, intractable hiccups) - Commonly used to tx insomnia and neuropathic pain - Adverse Effects: Overexpression of therapeutic - Have been known as tranquilizers or neuroleptics - Contraindications: Known drug allergy, pregnancy, recent MI effects - Adverse Effects: Dry mouth, constipation, blurred vision, urinary retention, dysrhythmias - Decreased CNS activity, sedation, HoTN, - Conventional/1st-gen: Phenothiazines drowsiness, loss of coordination, dizziness, - 2nd-gen: Atypical Antipsychotics headaches, N/V, dry mouth, constipation, Indications: Monoamine oxidase inhibitors (MAOIs): others - Psychotic illness, most commonly schizophrenia Selegiline Transdermal Patch (Emsam) - Overdose: Dangerous when taken w/ other - Anxiety and mood disorders