Pharma Week 8 Midterms.pdf

J U C C CENTRAL NERVOUS SYTEM DRUGS stimulants STIMULANTS CNS Stimulants medically approved use of these drugs is limited to the treatment of attention deficit/hyperactivity disorder (ADHD) in children, narcolepsy, obesity and the reversal of respiratory distress...

J U C C CENTRAL NERVOUS SYTEM DRUGS stimulants STIMULANTS CNS Stimulants medically approved use of these drugs is limited to the treatment of attention deficit/hyperactivity disorder (ADHD) in children, narcolepsy, obesity and the reversal of respiratory distress Major group: 1. Amphetamines – stimulate the cerebral cortex of the brain 2. Analeptics – act on the brain stem to stimulate respirationBreathing 3. Anorexiants – act to some degree on the cerebral cortex & on the 0 hypothalamus to suppress appetite NARCOLEPSY falling asleep during normal waking activities such as driving a car or talking with someone a chronic neurological disorder caused by the brain’s 0 inability to regulate sleep-wake cycles normally ADHD (Attention Deficit/Hyperactivity Disorder might be caused by a disregulation of transmitters serotonin, norepinephrine & dopamine SNIinability to concentrate, behaviors include inattentiveness, restlessness (fidgety), hyperactivity (excessive & purposeless activity), inability to complete tasks & impulsivity more common in boys than in girls In ADHD, it is believed that there is decreased levels of dopamine and norepinephrine in the prefrontal cortex circuits. 080 All ADHD medication aim to increase the levels of the hormones. 1. Amphetamines - stimulates the release of the neurotransmitters norepinephrine and dopamine from the brain and sympathetic nervous system - excessive use may lead to psychosis - may cause euphoria, increase alertness, xerostomia (oral dryness), insomnia, restlessness, irritability and weight loss.  METHYLPHENIDATE (Ritalin) C Stimulant; used to increase attention span in child with ADHD H Decreased hyperactivity E O Best taken 30 minutes to 1 hour before meals, usually before breakfast. Is stomach upset occurs, take it with or after meals. Note that taking it with meals alters its metabolism and absorption. Give it in the morning or at least 6 hours before bedtime since it causes insomnia C May cause growth retardation K Monitor growth and development  AMPHETAMINE & AMPHETAMINE LIKE DRUGS Dextroampheta For narcolepsy, ADHD, obesity. May cause euphoria, confusion, mine sulfate anorexia, abdominal pain, wt loss, growth suppression, palpitations, tachycardia, HPN and erectile dysfunction Modafinil For narcolepsy, ADHD, shift work sleep disorder and sleep apnea, May cause headache, dizziness anxiety, anorexia, dry mouth, insomnia, rhinitis, back pain Dexmethylpheni For ADHD. May cause dizziness, restlessness, anxiety anorexia, date HCL nausea, dry mouth abdominal pain, nasal congestion. May cause sudden death in patients with structural cardiac abnormalities Pitolisant For excessive daytime sleepiness associated with narcolepsy. (dobutamine-3 May cause headache anxiety nausea, infection ad receptor musculoskeletal pain antagonist) 2. Analeptics - CNS stimulants mostly affects the brainstem, spinal cord and cerebral cortex - primary use of analeptics is to stimulate respiration Side effects and adverse reaction: restlessness, tremors, palpitations, tachycardia, insomnia, GI irritation and urinary frequency 3. Anorexiants - cause a stimulant effect on the hypothalamic and limbic regions 0 of the brain to suppress appetite - long term use may cause severe side effects such as euphoria, restlessness, palpitations, tachycardia, erectile dysfunction and HPN Contraindications: HPN, hyperthyroidism, glaucoma, within 14 days of MAOI therapy & children below 12 yrs old Benzphetamine Short-term (8-12wk) treatment for obesity, may cause HCL dizziness, restlessness, headache, insomia, dry mouth dysgeusia Naltrexone Used short term obesity, headache dizziness, insomnia, HCL/bupropion vomiting, suicidal ideation, HPN and erectile dysfunction HCL Caffeine citrate For neonatal apnea and mental alertness. May cause headache, (methylxanthines insomnia, nausea, tachycardia, palpitations and urinary ) frequency Theophylline For airway obstruction and bronchospasm prophylaxis. May cause headache, insomnia, vomiting, seizure, dysrhythmia, hypokalemia, hypercalcemia, tachycardia CNS Depressants - cause varying degrees of depression (reduction in functional activity) within the CNS Broad Classifications: 1. Sedative-Hypnotics 2. General & Local Anesthetics 3. Analgesics 4. Anticonvulsants 5. Antipsychotics 6. Antidepressants Sedative-hypnotic - commonly ordered for treatment of sleep disorders I_ The mildest form of CNS depression is sedation which diminishes physical and mental responses at lower dosages but does not affect consciousness and increasing the drug can cause hypnotic effect (form of natural sleep) I 8 - Hypnotic drug therapy should usually be short term to prevent drug dependence and tolerance but abruptly discontinuing a high dose hypnotic can cause *withdrawal symptoms *trembling & tremors, muscle pain or aches, hunger or loss of appetite, fatigue, sweating, irritability & agitation, depression, anxiety, nausea, vomiting, confusion, paranoia, seizures & dilated pupils 2 types: a. Short-Acting Hypnotics – useful in achieving sleep because they allow client to awaken early in the morning without experiencing lingering side effects b. Intermediate Acting Hypnotics – useful for sustaining sleep, however, the client may experience residual drowsiness or hangover in the morning Categories: 1. barbiturates 2. benzodiazepines 3. nonbenzodizepines  1. BARBITURATES Short acting: For sedation induction and insomnia. Effectiveness is lost Secobarbital within 2 weeks. May cause confusion, drowsiness, Sodium constipation, withdrawal, sleep-related behaviors, nightmares and suicidal ideation Intermediate To manage anxiety, sedation induction, and insomnia, use acting: short term and avoid alcohol with all barbiturates. May cause Butabarbital ataxia, drowsiness, sleep relate disorders, agitation, Sodium hypotension, depression and angioedema. This drug is no longer accepted for use in older adults or debilitated adult patient with insomnia. Long acting: Used for seizure control, sedation induction and insomnia. May Phenobarbital cause ataxia, depression, bradycardia, hypotension, dizziness, confusion, drowsiness impaired judgement. Monitor of respiratory depression 2. BENZODIAZEPINES - Minor tranquilizer or anxiolytic (antianxiety agent) - flurazepam (Dalmane), estazolam (ProSom), quazepam (Doral), diazepam (Valium), clonazepam (Klonopin), alprazolam (Xanax), lorazepam (Ativan) & temazepam (Restoril) - Classified as schedule IV - Can suppress stage 4 of NREM (non rapid eye movement) sleep, which may result in vivid dreams or nightmares and can delay REM(rapid eye movement) sleep - Should not be used for longer than 3-4 weeks as a hypnotic flumazenil – benzodiazepine antagonist; for cases of overdose  FLURAZEPAM C Short term treatment for insomnia H Increased sleep duration and decreased nocturnal awakening due to the hypnotic effect from CNS depression E Maybe taken without regards to meal C Advise against smoking; alcohol and abrupt withdrawal of the medication Side effects: drowsiness and ataxia (lack of balance & coordination) Effect after discontinuation: possible disturbed sleeping pattern for 1-2 nights after discontinuing K Symptoms of abrupt withdrawal after long term use: restlessness, hand tremors, muscle cramps, vomiting, diaphoresis Antidote: Flumazenil Lorazepam Used for sedation induction and to reduce anxiety. Should not be used for more than 6 weeks. May cause tolerance dizziness, E drowsiness, anterograde amnesia, confusion, ataxia, edema, dependence, withdrawal Triazolam To management of insomnia. Should not be used longer than 7-10 weeks at a time to avoid tolerance. Avoid alcohol, smoking when taking triazolam. May cause tolerance, drowsiness, ataxia, confusion, to visual impairment, tachycardia, depression, anterograde amnesia Nonbenzodiazepines: For ultrashort term treatment of insomnia. May cause headache Zaleplon dizziness, drowsiness, abdominal pain and sleep related disorders Opioid Agonist: For general anesthesia induction and sedation maintenance. Use Alfentanil cautiously in patient with head trauma and liver dysfunction. May of cause dizziness, confusion, dysrhythmias, respiratory depression, hypotension or HPN chest wall rigidity Opioid agonist: For general anesthesia and maintenance and moderate to sever pain. Remifentanil May cause dizziness, pruritus, confusion, chest wall rigidity, bradycardia, dysrhythmia Nonbenzodiazepine 1. Zolpidem (Ambien) - a non-benzodiazepine that differs in chemical structure from benzodiazepines - used for short term treatment 2. Ramelteon - newest category of sedative-hypnotics - a melatonin agonist for sleep disorders - not classified as a controlled substance and it acts by selectively targeting melatonin receptors to regulate *circadian rhythms - the only major sedative hypnotic approved for treating chronic insomnia *circadian rhythm – the 24 hour internal clock in the brain that regulates cycle of alertness & sleepiness by responding to light changes in our environment C Sedative o ZOLPIDEM H Adequate Sleep E Best taken 30 mins to 1 hour before bedtime C Do not take it long term Side Effects: drowsiness, blurred vision, lethargy, headache, palpitations Adverse effect: Leukopenia & granulocytopenia (low WBC) Life threatening: pulmonary edema, renal failure K Avoid driving, alcohol Take small frequent feeding Activated charcoal is used to treat overdose Check: ALT, AST (test in assessing liver)  ESZOPICLONE (Lunesta) C Treatment for insomnia H Increased sleep duration and decreased nocturnal awakening due to the hypnotic effect from CNS depression E Best administered immediately before bedtime C Do not give with or immediately following a high fat or heavy meal Advise against alcohol intake; instruct the patient to have at least 8 hours allotted for sleep before the start of daily activity Side effects: unpleasant taste and headache K Report worsening insomnia that persist for more than 7-10 days. Presence of abnormal thoughts or behavior, memory loss or anxiety stimulants ANESTHETICS Anesthetics - use to prevent pain during surgery & other procedures 2 main types: 1. General Anesthetics – depress the CNS, alleviate pain & causes loss of consciousness a. Balanced anesthesia - a combination of drug frequently used in general anesthesia - hypnotic given the night before surgery, premedication of narcotic analgesic to decrease secretion, short-acting barbiturate, inhaled gas & muscle relaxant as needed - because of lesser general anesthetics given, there are fewer adverse reactions b. Inhalation Anesthetics – gas or volatile liquids administered as gas - used to deliver general anesthesia ex. Nitrous oxide – “laughing gas”; was the first anesthetic (1800) c. Intravenous Anesthesia – for the induction stage of anesthesia; have rapid onsets & short duration of action ex. droperidol (Innovar) ketamine hydrochloride (Ketalar) 2. Local Anesthetics- block pain at the site where the drug is administered allowing consciousness to be maintained - for dental procedures, suturing skin lacerations, performing short- term (minor) surgery at a localized area & for diagnostic procedures such as lumbar puncture & thoracentesis a. short acting – ½ to 1 hour; Procaine hydrochloride (Novocain) b. moderate acting – 1 to 3 hours; Lidocaine hydrochloride (Xylocaine) c. long acting – 3 to 10 hours; etidocaine (Duranest) Topical Anesthetics – limited to mucous membranes, broken or unbroken skin surfaces and burns; decreases the sensitive nerve endings of the affected area - could be in solution, liquid spray, ointment, cream & gel ex. Xylocaine Gel, Lidoderm, lidocaine Spinal Anesthesia- local anesthetic injected in the subarachnoid space at the 3rd or 4rth lumbar space (L3 to L4) - encourage the patient to remain flat on bed after surgery various sites of the spinal column: Spinal block – the penetration of the anesthetic into the subarachnoid membrane a. Epidural block- placement of local anesthetic in the outer covering of the spinal cord, or the dura matter b. Caudal block- an epidural block placed by administering anesthetic in sacral hiatus c. Saddle block- given at the lower end of spinal column to block the perineal area EPIDURAL BLOCK CAUDAL BLOCK  Stages of anesthesia 1 0 0 Analgesia: Begins with consciousness and ends with loss of 0 consciousness, speech is difficult, sensations of smell and pain are lost, 0 dreams and auditory visual hallucinations may occur. May be called 8 induction stage Excitement of delirium: produces a loss of consciousness caused by 2 depression of the cerebral cortex, confusion, excitement or delirium occur and induction time is short Surgical: Surgical procedure is performed during this stage. As anesthesia 3 00 deepens, respirations become shallower and the respiratory rate is increased Medullary paralysis: toxic stage of anesthesia in which respirations are 4 lost, and circulatory collapse occur, ventilatory assistance is necessary  Anesthetics: Inhalation Halothane Contraindicated in obstetrics, recovery is rapid, could decrease blood pressure Isoflurane Frequently used in inhalation therapy, has a smooth and rapid induction of anesthesia and rapid recovery. This drug should not be used during labor because it suppresses uterine contractions. cardiovascular effect is minimal Sevoflurane For induction and maintenance during surgery. Sevoflurane may be given alone or combined with nitrous oxide Desflurane Volatile anesthetic, recovery is rapid after anesthetic administration has ceased. Could cause hypotension and respiratory depression Inhalation Must be administered at no less than a mixture of oxygen; potency is low. Recovery is rapid with minimal cardiovascular effect gas(nitrous oxide)  Intravenous anesthetics Benzodiazepines Diazepam For induction of anesthesia, no analgesic effect Midazolam For induction of anesthesia and for endoscopic procedure. Can cause conscious sedation and should be avoided if cardiopulmonary disorder is present Fentanyl For neuroleptic analgesic used with a general anesthesia, can also be used as pre-anesthetic drug and also used for diagnostic procedure. May cause hypotension and respiratory depression Ketamine Used for short term surgery or for induction of anesthesia, increases salivation, BP and heart rate. Avoid in patients with psychiatric disorders Propofol For induction of anesthesia; maybe used with GA, duration of action is short, may cause respiratory depression and hypotension. Pain can occur at the injection site.  Midazolam C Sedative, Hypnotic, Antidepressant H Prevention of convulsions and muscle spasms. Promote muscle relaxation; for acute repetitive seizures E Take as prescribed C Avoid alcoholic beverages; Side effects: drowsiness, weakness, nausea, vomiting, confusion K Avoid driving; avoid intake of grapefruit juice Do no use long term basis; may cause independence  Local anesthetics Short For nerve block, infiltration, epidural and spinal anesthesia, useful in acting:30min-1hr-procain dentistry; e hydrochloride Short acting: For infiltration, caudal and epidural anesthesia. Onset of action is 6-12 Chloroprocaine HCL minutes Moderate acting(1-3hr) For nerve block, infiltration and spinal anesthesia. Lidocaine is used to lidocaine HCL treat cardiac dysrhythmias Moderate acting: For peripheral nerve block, infiltration, caudal and epidural anesthesia Prilocaine HCL Long acting(3-10hr): For peripheral nerve block, infiltration, caudal and epidural Bupivacaine HCL Dibucaine HCL For topical use Tetracaine HCL For spinal anesthesia,(high and low saddle) local use includes usage in the eye to anesthetized the cornea, the nose and throat for bronchoscopy and skin for relief of pruritus ANTICONVULSANTS Anticonvulsants/Antiseizure/Antiepileptic drugs used for epileptic seizures stabilize nerve cell membranes and suppress the abnormal electric impulses in the cerebral cortex also classified as CNS depressants Epilepsy – a seizure disorder due to an abnormal electric discharges from the cerebral neurons and is characterized by a loss or disturbance of consciousness and usually by a convulsion. - causes: fever, hypoglycemic reaction, electrolyte imbalance, acid-base imbalance, alcohol or drug withdrawal, head trauma, congenital malformations, tumors while some are unknown Action of Anticonvulsants 1. Supressing the sodium influx 2. Supressing calcium influx 3. Increasing the action of GABA – inhibits the neurotransmitters throughout the brain  Drug on Focus: Phenytoin (Dilantin) C Anticonvulsant H Prevention of seizures E Best taken with food to enhance absorption C Massage the gums, it causes gingival hypertrophy May turn the urine pink, red or reddish brown K Monitor for signs and symptoms of bone marrow depression Do not discontinue abruptly, taper of in two weeks Use saline flush before and after IV administration Report skin rash Drug-food-lab interaction: increase effects with Pharmacodynamics: Oral: slowly absorbed cimetidine, isoniazid, chloramphenicol.; decreased IM: erratic rate of absorption effects with folic acid, calcium, antacids; decreased Metabolism: t ½ 7-60h effects of anticoagulants, oral contraceptives, Excretion: in urine, in bile, feces antihistamines and corticosteroids, theophylline, dopamine and repamfin. Side effects: confusion; drowsiness, insomnia, Adverse reaction: hypotension, hyperglycemia, nervousness, asthenia, slurred speech, ataxia, rash, peripheral neuropathy, purple glove syndrome dysgeusia, tremor, hyperreflextion Life threatening: agranulocytosis, leukopenia, thrombocytopenia, suicidal ideation, steven johnsn syndrome  Drug on focus: Lamictal (Lamotrigine) C Treatment of seizures, epilepsy and bipolar disorder I H Prevention of seizures, decreased hyperactivity in bipolar disorder I E Maybe taken with or without food C Side effects: rashes- Steven’s Johnson syndrome K Withhold if patient has allergy’ check CBC, platelets; Do not withdraw abruptly Drug on focus: Carbamazepine (Tegretol) C Anticonvulsant; used in management of seizures H Prevention of convulsions or seizures E Best taken with food or milk to decrease GI upset C Avoid: 1. driving and other activities requiring alertness within the first 3 days 2. Do not abrupt withdrawal; discontinue gradually 3. Avoid with use of alcohol K Myelosuppresion, ataxia, photosensitivity may result, Urine may turn pink to brown, Monitor blood levels (CBC)  Drug on focus: Topiramate (Topamax) C Anticonvulsant, use in management of seizures H Prevention of convulsion E Taken without regard to melas; open capsules and can be mixed or sprinkle in juice C Side effects: Dizziness, drowsiness, wt. loss, vision problem, ataxia, diplopia, rash Use sunscreen an protective clothing to prevent photosensitivity Use caution with hazardous activity Increase fluid intake to prevent formation of kidney stones K Avoid abrupt withdrawal Stop drug immediately if eye problems occurs Wear medication information tag Phenobarbital For tonic-clonic, myoclonic and partial seizures, status epilepticus; sedation induction; anxiety and insomnia, May cause dizziness, drowsiness, weakness, headache, confusion, ataxia, hypotension and erectile dysfunction Clonazepam For absence and myoclonic seizure and panic disorder. May cause drowsiness, ataxia fatigue, dependence, depression, memory impairment, infection, and respiratory depression Diazepam Drug if choice for status epilepticus; partial and tonic-clonic seizure, muscle spasm and anxiety, sedation induction and alcohol withdrawal. May cause wt gain/loss, appetite stimulation, urinary retention/incontinence, menstrual irregularity. Administer slowly to avoid respiratory depression and hypotension Lorazepam To control status epilepticus, anxiety and insomnia, and for sedation induction. May cause dizziness, drowsiness, memory impairment, confusion, constipation, injection site reaction Oxcarbazepine For partial seizures, may cause dizziness, drowsiness, confusion, ataxia, rhinitis infection and visual impairment Ethosuximide For absence seizure, May cause headache, ataxia, nightmares, impared cognition, diplopia, nausea vomiting Valproic Acid For seizure prophylaxis, for partial, myoclonic, absence and tonic-clonic seizure, bipolar disorder, migraine prophylaxis. May cause dizziness, drowsiness, weakness, diplopia, insomnia, anorexia abdominal pain, dyspepsia Acetazolamide For absence seizures, altitude sickness, glaucoma and edema. Maintain adequate fluid intake to prevent renal impairment. May cause confusion, depression, ataxia, flushing, diarrhea and crystalluria Tiagabine For partial seizures, May cause euphoria, diarrhea, pharyngitis, infection Topiramate For partial and tonic-clonic seizure, Lennoux-Gastaut syndrome and migraine prophylaxis, May cause nystagmus, infection fatigue, diplopia, irritability anorexia Pregabalin For neuropathic pain, partial seizures, fibromyalgia. May cause confusion drowsiness, peripheral edema, xerostomia, appetite stimulation Felbamate For partial seizure and Lennoux-Gastaut syndrome. May cause dizziness, drowsiness, anxiety paresthesia, dyspepsia, diarrhea, vomiting