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NURS 251 Pharmacology Final Exam Module 10-comprehensive-2023-2024 Opioid Tolerance: Develops for euphoria, respiratory depression, nausea. Does NOT develop for constipation or miosis. Opioid Physical Dependence: Substantial for opioids. Abstinence syndrome extremely unpleasant but rarely dangerous. Protracted withdrawal may persist for months and characterized by insomnia, irritability and fatigue.
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Opioid Tolerance: Develops for euphoria, respiratory depression, nausea. Does NOT develop for constipation or miosis. Opioid Physical Dependence: Substantial for opioids. Abstinence syndrome extremely unpleasant but rarely dangerous. Protracted withdrawal may persist for months and characterized by insomnia, irritability and fatigue. OUD Maintenance Therapy Opioid Overdose Reversal Drug Class Pure Opioid Agonist Partial Mu Agonist, Kappa Antagonist Pure Opioid Antagonist Pure Opioid Antagonist Prototype Methadone Buprenorphine Naltrexone Naloxone MOA Replaces/substitutes the misused opioid Replaces/substitutes the misused opioid Discourages opioid use by blocking euphoria/effects Reverses respiratory and CNS depression Therapeutic Uses OUD withdrawal/detox, OUD maintenance/suppressive therapy, pain management OUD withdrawal/detox, OUD maintenance/suppressive therapy, pain management AUD, OUD (after detox) Reversal agent for overdose, post-op effects, neonate resp. depression AEs Standard opioid AEs; QT prolongation; respiratory depression ; hepatic injury HA; GI upset; anxiety; sleep disturbances; LE edema; sweating GI; HA, sedation, anxiety; injection-site rxns; liver toxicity Reversal of pain control, withdrawal if physically dependent on opioids Nursing Implications CII Controlled Substance Baseline ECG, routine thereafter for cardiac hx; report sx of liver injury; monitor VS and dose sufficiency to suppress withdrawal Greater risk of death if relapse after discontinuation 𝖳 effectiveness with counseling CIII Controlled Substance Administer tablets and film sublingually Greater risk of death if relapse after discontinuation 𝖳 effectiveness with counseling MUST be opioid-free (- urine) Manufacturer provided needles in gluteal muscle Greater risk of death if relapse after discontinuation 𝖳 effectiveness with counseling Titrate carefully to prevent withdrawal/loss of pain control Monitor for 4+hrs after overdose Teach proper admin technique based on product prescribed Other PK: LONG half-life and duration of action , cross tolerance to other opioids IV: PMH/FH of QT prolongation. May be used in pregnancy DDIs: CNS depressants, QT-prolonging drugs, CYP3A4 inhibitors Safety: Accumulation/respiratory depression with repeat dosing, only prescribed for OUD through opioid tx program (exception for 72hrs of IP use) IV: PMH/FH of QT prolongation. PREFERRED in pregnancy alone. DDIs: Strong inducer/inhibitors of CYP3A4, CNS depressants Safety: Ceiling effect : lower abuse/respiratory depression (𝖳 with concomitant CNS depressants ) IV: contraindicated in acute hepatitis/liver failure; NOT used in pregnancy DF: Monthly IM injection. Preferred in OUD DDIs: Opioids (no others) Pain management may be difficult given drug properties Can precipitate withdrawal PK: SHORT half-life, onset 2- 5mins, duration; hours, STRONG mu binding, NOT PO (1st^ pass) DF: SubQ/IM/IV, IN DDIs: opioids Can precipitate withdrawal Opioid Overdose Risk Factors*
cologne, etc. AUD: Chronic, relapsing disorder characterized by: impaired control over drinking, preoccupation with consumption, use of alcohol despite awareness of adverse consequences, distortions in thinking, esp. aeb denial of problem. Influenced by genetics, psychosocial, and environmental factors. May lead to psychological issues, malnutrition, poor work performance, family/social deterioration, and health consequences. Alcohol Withdrawal Syndrome: Begins 4 - 12hrs after last drink. May continue for 5 - 7 days. [N/V, tremors, restlessness, insomnia, depression, irritability, 𝖳 HR/BP/temp/RR, diaphoresis, seizures, illusions] Alcohol Withdrawal Delirium: 2 - 3 days after abrupt withdrawal. < MEDICAL EMERGENCY Withdrawal Maintenance Drug Class Benzodiazepines Aversion Therapy Pure Opioid Antagonist Prototype Disulfiram Naltrexone Acamprosate MOA Disrupts alcohol metabolism, irreversible inhibition of aldehyde dehydrogenase ¯ Cravings/blocks reinforcing (pleasurable) effects Reduces unpleasant feelings associated with abstinence Therapeutic Uses AUD (^) SEE PREVIOUS CHART. Tablets administered daily (option for AUD) Mouthwash, cough syrup,
AEs W/ Alcohol: Acetaldehyde Syndrome {Mild: N/V, flushing, palpitations, HA, sweating, thirst, hypotension. Severe: resp. dep., CV collapse, dysrhythmias, seizures, death} W/out Alcohol: rash; drowsiness; liver dysfunction (rare); peripheral/optic neuritis (rare) Diarrhea; suicide-related events (rare) Nursing Implications Admin no sooner than 12 hours after last drink High quality patient education (effects persist 2 weeks after d/c, medical alert bracelet ) Give with meals tid ; Start after detox is over (~5 days after cessation) ; evaluate renal function; 𝖳 effectiveness with counseling Other IV: heart disease, hepatic dysfunction, psychiatric disorders DDIs: alcohol, metronidazole, warfarin Safety: avoid alcohol containing products DF: tablets tid IV: ESRD or CrCl < 30mL/min; avoid in pregnancy
Anxiolytics Prototype MOA (^) Therapeutic Uses AEs (^) Nursing Implications Other Other Drugs Used GAD Buspirone Anxiolytic properties, activity at serotonin receptors NonBZD- Nonbarbiturate Anxiolytic only. Takes weeks to see effects Dizziness; nausea; HA; drowsiness Supportive, biofeedback therapy, relaxation training DDIs: ketoconazole, erythromycin, grapefruit juice No tolerance issues, no CNS effects (safe with other CNS depressants) BZDs (Diazepam), antidepressants (SSRIs/SNRIs) Panic Disorder SSRIs (DOC) Best with combo therapy (CBT/drug) BZDs effective (not used alone); TCAs/MAOIs effective (adverse effects) OCD SSRIs (DOC) Continue therapy for at least 1 yr before d/c Social Anxiety SSRIs (DOC) (^) Used in lower doses than with depression BZDs, [propranolol/BBs for performance anxiety] PTSD SSRIs, SNRIs Stimulants Prototype Amphetamine/Dextroamphetamine Methylphenidate (Amphetamine-like) Atomoxetine (non-stimulant) MOA Promote NE and DA release, inhibit reuptake Promote NE and DA release, inhibit reuptake Selective inhibitor of NE reuptake Therapeutic Uses ADHD, narcolepsy ADHD, narcolepsy ADHD (2nd^ line) AEs CNS stimulation; weight loss; HA; abdominal pain; lethargy OD: dizziness, confusion, hallucinations, paranoid delusions, palpitations, dysrhythmias, HTN CNS stimulation; HA; abdominal pain; lethargy OD: dizziness, confusion, hallucinations, paranoid delusions, palpitations, dysrhythmias, HTN GI rxns, allergic rxns (angioneurotic edema); suicidal thoughts; weight loss; growth delay ; severe liver injury Nursing Implications CII Controlled Substance (tolerance, dependence) Take dose after breakfast and last dose before 4pm CII Controlled Substance (tolerance, dependence) Take dose after breakfast and last dose before 4pm NOT Controlled Substance Other IV: contra in patients with symptomatic CVD Safety: withdrawal sx with abrupt d/c ; OD; DF confusion (IR, SR, ER), patch hypersensitivity IV: contra in patients with symptomatic CVD Safety: withdrawal sx with abrupt d/c ; OD; DF confusion (IR, SR, ER), patch hypersensitivity DDIs: MAOIs
Antidepressants Drug Class Prototype MOA Therapeutic Uses AEs Nursing Implications Other SSRIs Fluoxetine Block neuronal serotonin reuptake Major depression, BPD, bulimia, premenstrual dysphoric disorder, anxiety/panic disorders Sexual dysfunction; insomnia; weight gain; serotonin syndrome ; neonatal effects, withdrawal syndrome Take early to prevent insomnia Methods to avoid AEs/DDIs Risk for suicidal ideation DDIs: MAOIs, TCAs, SNRIs, St. Johns Wort (𝖳 serotonin syndrome ); strong inhibitor of CYP2D SNRIs Venlafaxine Block neuronal serotonin/NE reuptake Major depression, anxiety, panic disorders, pain HTN, tachycardia; sexual dysfunction; insomnia; weight loss; serotonin syndrome; withdrawal syndrome ; bronchitis/dyspnea; CNS effects, neonatal effects Take early to prevent insomnia Methods to avoid AEs/DDIs (monitor BP) Risk for suicidal ideation DDIs: MAOIs, TCAs, SNRIs, St. Johns Wort (𝖳 serotonin syndrome ); CNS depressants Atypical Buproprion Blocks DA/NE reuptake Major depression, prevent SAD, smoking cessation (Zyban) Insomnia, seizures; HTN, tachycardia IV: 𝖳^ risk of seizure in pt with seizure hx or eating disorder DDIs: MAOIs, 2D inhibitors ( 𝖳 seizures) TCAs Amitriptyline Blocks uptake of monoamine transmitters (NE/serotonin) Depression, BPD. Fibromyalgia/pain, insomnia, ADHD, anxiety/panic disorders Anticholinergic effects, orthostatic hypotension, sedation ; arrhythmias/seizures (can be lethal in OD) Give at bedtime Methods to avoid AEs/DDIs Lethal dose only 8x average therapeutic dose OD tx: gastric lavage/activated charcoal; IV bicarb for dysrhythmias DDIs: MANY!! Other antidepressants Safety: OD. No more than 1 week supply for OP depressed pt MAOIs Phenelzine Prevents conversion of MAO-A, 𝖳 NE, serotonin, DA, tyramine in brain Major depression, bulimia, panic/anxiety disorders Hypertensive crisis in combo with high tyramine foods ; CNS stimulation, orthostatic hypotension Warn of risks of DDIs/high tyramine foods (give pt a list) [aged cheeses, pickled meats, red wine, fava beans] DDIs: MANY!!; Other antidepressants Inhibition lasts ~14 days after drug is d/c CAMs St. John’s Wort No more effective than placebo for MDD tx Mild, photosensitization, serotonin syndrome with other ADs Lack of standardization/quality of product can be a problem DDIs: CYP450 enzyme inducer , PGP inducer
Antipsychotics Drug Class First Generation Antipyschotics Second Generation Antipyschotics Prototype Haloperidol Risperidone Clozapine MOA Block dopamine receptors in the mesolimbic area of the brain Blocks dopamine (less) and serotonin (more) receptors (^) Clozapine is usually avoided due to risk of agranulocytosis Therapeutic Uses Schizophrenia (positive sx), psychosis, Tourette’s (DOC) Schizophrenia, BPD, levodopa-induced psychosis AEs Extrapyramidal Sx (acute dystonia, akathisia, Parkinsonism, [early in tx w/ 𝖳 potency FGAs] tardive dyskinesia); Neuroleptic Malignant Syndrome Anticholinergic; orthostatic hypotension; sedation; severe dysrhythmias; neuroendocrine; seizures; agranulocytosis ; sexual dysfunction; dementia (OA) Metabolic effects: weight gain, new onset diabetes, dyslipidemia Rare: seizures, EPS , agranulocytosis , myocarditis, orthostatic hypotension, dementia (OA) Nursing Implications Identify high risk pts (on QT drugs) Promote adherence Educate; sx of early/late EPS report to provider ASAP , agranulocytosis (fever, sore throat) Observe for NMS, take action quickly Measure baseline BMI, every visit for 6 months, then q3mos after. FBS at baseline, 12 weeks, then annually Fasting lipid profile at baseline and q6mos Identify high-risk pts (diabetics) , promote adherence Educate; sx of early/late EPS report to provider ASAP , agranulocytosis, metabolic effects Other DF: PO, IV, IM, Depot IM IV: Contra in pts on QT drugs DF: tablets, orally disintegrating tablets, IM depot Oral therapy with IM therapy for first 3 weeks
Sudden, often dramatic contractions of skeletal muscle groups; often involving head, neck, back, laryngeal muscles. Early: Develops within 24- 96hr of therapy initiation/dose increase. MEDICAL EMERGENCY- Tx with anticholinergic agents such as diphenhydramine (IV or IM) or benztropine (IM)
Stiffness, shuffling gait, pill rolling, mask-like faces, cog- wheeling at elbow, drooling. Early: Develops within 1st month of therapy Tx: decrease antipsychotic dose or use oral anticholinergics
Inability to sit still, urge to move about; easily mistaken for 𝖳 anxiety and agitation. Early: Develops within first 2 months of therapy Tx: Less responsive to anticholinergics. May respond to in antipsychotic dose or switching to a low potency antipsychotic. Admin of BB or BZD ( propranolol is DOC b/c of lipid solubility allowing it to cross BBB
Rhythmic involuntary movements of tongue, lips, or jaws No reliable management, prevention is key [Use FGAs in lowest effective dose for shortest duration] Late: Monitor for TD q3mos after initial 12 mos of therapy SGAs: clozapine and quetiapine decreased risk of TD Neuroleptic Malignant Syndrome Can occur with any antipsychotic agent, most concerning with 𝖳 potency FGAs. Sx evolve over 24-72hrs (temp> 38°C, autonomic dysfunction, lead pipe rigidity, altered conscious, seizures, coma) Tx: d/c, supportive (cooling blankets, antipyretics) Dantrolene, bromocriptine, BZDs
Cardinal Parkinson’s Symptoms: Tremor, rigidity, postural instability, slowed movement Early Parkinson’s Symptoms: Worsening of handwriting, clumsiness, shakiness, slower gait, loss of smell, excessive salivation Late Parkinson’s Symptoms: Resting tremor, rigidity, bradykinesia, postural instability Nonmotor Symptoms: Autonomic sx, sleep disturbances, depression, dementia, psychosis Parkinson’s Drugs Drug Class Dopamine Replacement Dopamine Agonists COMT Inhibitors Anticholinergics Prototype Carbidopa/Levodopa Pramipexole Enta capone Benztropine MOA Levodopa converted to DA. Acts at DA receptors in CNS. Carbidopa inhibits decarboxylation of DA in intestine/peripheral tissues so more Levodopa reaches CNS Directly stimulates dopamine receptors Selective, reversible COMT inhibitor Block cholinergic receptors Therapeutic Uses PD [MOST EFFECTIVE] PD; restless leg syndrome Used only in combo with carbidopa/levodopa Used in early disease process to preserve response to Levodopa AEs N/V, hypotension ; CNS effects (confusion, hallucinations, depression), involuntary movements (excess DA in CNS) Confusion, hallucinations, nausea, orthostatic hypotension, somnolence, impulse control disorders Hallucinations; NV; dyskinesias Confusion, hallucinations; dry eyes; dry mouth; blurred vision; constipation; urinary retention Nursing Implications W/ food to reduce N/V (empty stomach preferred) DON’T admin with high-protein meals If onset delayed, give on empty stomach, crush/chew with full glass of water Educate: “on/off”, dyskinesias Abrupt d/c can be life threatening Educate: recognize and report AEs to provider Always admin with carbidopa/levodopa. Allows more levodopa to get to the brain. Educate on methods to minimize anticholinergic AEs Other (^) DDIs: FGAs, MAOIs Drug WEARS OFF at end of dosing interval IV: reduce dose for renal impairment DDIs: Methyldopa, Dobutamine, Isoproterenol IV: caution in pts with glaucoma
Valproic Acid Inhibits Na & Ca channels. Enhances GABA Epilepsy, BPD, migraines N/V, hepatotoxicity (jaundice, abd pain, anorexia), pancreatitis (NV, abd pain), birth defects , hyperammonemia (altered consc. Vomiting, lethargy) in combo with topiramate); alopecia Take with food to ¯ NV Monitor for breakthrough seizures if carbapenems initiated Monitor for hepatotoxicity, pancreatitis, hyperammonemia DF: Multiple salt forms (valproic acid, valproate, divalproex sodium) IV: avoid in children < 2yrs, avoid in pre-existing liver dysfunction DDIs: phenytoin toxicity when used in combo; carbapenem abx levels Newer AEDs Oxcarbazepine Inhibits Na channels Epilepsy CNS: dizziness, drowsiness, HA, ataxia, nystagmus; Derm: rash, SJS, TEN ; hyponatremia; hypothyroidism Mild skin rxns tx with antihistamines d/c with serious skin rxn
Safety: Do not drive until know how affects pt, monitor serious skin rxn DDIs: oral contr., diuretics Lamotrigine Inhibits Na & Ca channels Epilepsy, BPD CNS: dizziness, diplopia, blurred vision; Skin: rash, SJS, TEN ; aseptic meningitis ; risk for suicide Requires SLOW titration when started to avoid life-threatening rash Levetiracetam Not well understood Epilepsy Drowsiness, weakness, aggression (particularly kids) Can use pyridoxine to mitigate aggression Safety: d/c if severe CNS effects occur Topiramate Inhibits Na & Ca channels, enhances GABA, inhibits glutamate receptors Epilepsy, BPD, neuropathic pain, migraine prophylaxis CNS: somnolence, dizziness, ataxia ; kidney stones; metabolic acidosis; hypohydrosis; angle-closure glaucoma Monitor blood bicarb levels Monitor glaucoma, periodic eye exams, monitor strenuous activity, report hyperventilation, fatigue, anorexia IV: avoid in pregnancy Status Epilepticus MEDICAL EMERGENCY that should be treated within 5 mins of seizure onset 1 st^ line therapy: BZDs Lorazepam preferred if IV access available Rectal diazepam or IN midazolam if no IV access Loading dose of levetiracetam, fosphenytoin, OR valproic acid Phenobarbital preferred in neonatal population
Asthma/COPD Drug Class Short Acting Beta Agonists Long Acting Beta Agonists Glucocorticoids Anticholinergic Drugs Prototype Albuterol Salmeterol Fluticasone / Salmeterol [Inhaled]: Beclomethasone [PO]: Prednisone Short Acting Long Acting Ipratropium Tiotropium Therapeutic Use PRN to abort asthma attack Prevent exercise induced asthma attack COPD Long-term control (should not be used as a monotherapy due to increased risk of death without corticosteroid) Acute exacerbation (Does NOT abort acute attack) Chronic management (administered every 12 hours) COPD, acute asthma exacerbation COPD, asthma (not 1 st^ line) Adverse Effects Beta 1 activity: tachycardia, arrhythmias Beta 2 activity: tremor, decreased K (high doses) Tolerance develops with frequent use Same as SABAs Inhaled: local effects, no serious toxicities Oral candidiasis, dysphonia, bone loss Oral: Adrenal suppression , osteoporosis, hyperglycemia, growth suppression Dry mouth Pharynx irritation Dry mouth Pharynx irritation Other NOT used for acute asthma attack Routes: inhalation, oral, intravenous Caveats: IV or PO use will have delayed anti-inflammatory action (6-8 hours). Inhaled for chronic management. Full ICS response seen after 2 - 4 weeks. Onset: 15min (longer than SABA) Duration: 4 - 6hr Onset: 30min Duration: 24hr
(Levemir) Degludec (Tresiba) Clear (^100) units/mL 200 units/mL Rx SubQ Insulin MOA Insulin Therapeutic Uses Promotes transport of glucose into muscle, liver, and adipose tissue Suppresses release of fatty acids from adipose tissue, preventing ketone formation Accelerates potassium uptake into muscles Promotes incorporation of amino acids into proteins Type I Diabetes Type II Diabetes if: Sx not controlled by diet/exercise or oral hypoglycemics During time of major stress or surgery Gestational diabetes, parenteral nutrition, hyperglycemic crisis (IV), hyperkalemia, Dx of GH deficiency Adverse Effects and DDIs Nursing Implications Hypoglycemia, lipohypertrophy (hardening by repeat injections in same place) DDIs: oral hypoglycemics, hyperglycemics, beta-blockers (mask sx of hypoglycemia such as tachycardia) HIGH ALERT DRUG Refrigerate unopened insulin, prefilled syringes needle up in refrigerator. Rotate within injection site. Monitor for AEs. Monitor blood sugar. HTN/HF/Angina Medications Prototype MOA Therapeutic Effects AEs Nursing Implications Other ACE-I Captopril/ Lisinopril Blocks enzyme HTN, HF, MI, Dry/hacking non- Take 1 hour before IV: ACE. Decreases nephropathy, productive cough, meals contraindications AFFECT RAAS production of diabetic angioedema , Seek treatment ASAP {pregnancy, SYSTEM angiotensin II and retinopathy hyperkalemia , increased for s/sx of bilateral renal aldosterone serum Cr, teratogenic (2nd^ angioedema artery stenosis, hx release and 3 rd^ trimester) of angioedema} Safety: angioedema pts NEVER take ACE I again Beta Blockers HIGH ALERT MED Dose conversion PO to IV d/t high first pass effect Propranolol [NS] Metoprolol [S] P: B1/2 blockade M: B1 blockade Decrease BP by decreasing renin release. Increased peripheral resistance blocking B2.
angina, control HR, migraine prophylaxis M: HTN, angina, HF, MI P: bradycardia, AV block, bronchospasm, CNS effects M: bradycardia, AV block, rebound cardiac excitation after abrupt d/c, HF P: Monitor HR and BP M: warn patients about abrupt d/c DDIs: CCBs (additive heart block) IV: HF, asthma NR: “-olol, - alol, ilol”
Non- dihydropyridines [CCBs] Verapamil Blocks calcium channels in blood vessels AND heart {vasodilation, increased coronary perfusion, decreased BP, contractility, and HTN, angina, dysrhythmias Constipation , dizziness, flushing, HA, partial/complete AV block Avoid grapefruit juice Take at night IV: never use in patients with sick sinus syndrome or 2 nd/3rd^ degree heart block DFIs: Grapefruit juice (inhibits metabolism) Safety: IR/SR Dihydropyridines Nifedipine Blocks calcium HTN, Angina Reflex tachycardia (IR) , Warn patients about [CCBs] channels in blood (vasospastic flushing, HA, dizziness, peripheral edema vessels (vascular angina with a peripheral edema, Do not crush ER (can smooth muscle), BB) gingival hyperplasia be deadly) little to no effect on heart Organic Nitrates Nitroglycerin Acts directly on Stable, HA, orthostatic Use lowest effective Dosage forms: IV vascular smooth unstable, hypotension, reflex dose to prevent (highly lipid soluble, muscle to variant angina tachycardia , tolerance tolerance. half life 5 - 7mins), promote Vasodilator Long-acting formulas: SL, buccal, NG vasodilation 8 drug-free hours per spray, patch day DDI: hypotensive If angina appears at drugs (BB, CCB), night, use another phosphodiesterase drug like a BB type 5 inhibitors Cardiac monitoring (Viagra) with IV admin (special non- permeable tubing; light breakdown) Statins [KNOW THESE WELL] Prototype Atorvastatin MOA HMG-CoA Reductase Inhibitor (essential for synthesis of cholesterol by liver) Therapeutic Uses Hypercholesterolemia, primary and secondary prevention of cardiovascular events (MI survivors, DM patients) AEs Overall well tolerated Diarrhea, new-onset diabetes, myopathy, liver toxicity (rare)
monitoring Anticoagulated pts shouldn’t receive meds by IM route Educate: s/sx of bleeding, avoid OTC NSAIDs, electric razor and soft toothbrush recommended, s/sx of bleeding/thrombosis Education: proper injection technique ( rotate sites, don’t push out bubble ) Review and evaluate INR before admin TELL EVERYONE they are on warfarin. Other Fast onset, short duration (t1/2= 1.5hrs) Route: IV or SubQ ONLY CAUTION: rapid admin may cause hypotension IV: High likelihood of bleeding (hemophilia, active PUD, head trauma), severe liver/kidney disease DDIs: drugs affecting platelet function (NSAIDs, aspirin), other anticoagulants SAFETY: available in several strengths, admin with smart pump Longer half-life and duration than Route: Oral only UFH IV: pre-existing bleeding disorders, liver Route: SubQ ($$$] disease/alcoholism , poor compliance, IV: red M u o c n e it d or o i s n e : P if ed C i r a C tr l ic < , (^3) o (^0) b m es L e / , m pr i e n gnancy, mrenaalnl duytsrfiutinocntion NEVER use in pregnant pt DDIs: CYP3A4 & CYP2C9 inhibitors- SMX/TMP, metronidazole, amiodarone, etc MANY! DFIs: Vitamin K rich diets Narrow Therapeutic Index Antibiotics Drug Class Prototype MOA Therapeutic Uses AEs Nursing Implications Other Beta-lactams [Disrupt cell wall synthesis] Penicillins NEVER GIVE IM IV! Its not Penicillin G [Parenteral] Binds to PCN- binding proteins inhibiting cell wall synthesis and causing lysis Safest abx on the market since humans don’t have cell wall DOC for syphilis ; prophylaxis: syphilis, endocarditis, rheumatic fever Narrow spectrum [G] Hypersensitivity , n/v, renal impairment, hyperkalemia (high dose Pen G K), seizures Anxiety, hallucinations, confusion, palpitations (procaine) Monitor for 30mins after for allergy Not compatible with aminoglycosides (gentamicin) Education: take entire course, report s/sx of allergy, wear ID bracelet if allergic to PCNs DF: PO(PenVK), IV (PenG), IM (procaine/benzathine) IV: PCN/beta-lactam allergy, renal dysfunction Safety: IM and IV dose mixups. CNS toxicity in overdose/ renal dysfunction NR: “-cillin” Cephalosporins Cephalexin Inhibits effective synthesis of the bacterial cell wall resulting in lysis Gram+ organisms Hypersensitivity (PCN cross reactivity); NVD; C. difficile colitis (rare); bleeding, hemolytic anemia; seizures (high dose) NEVER combine Ca and ceftriaxone in IV , monitor for phlebitis Educate: full course, allergy, avoid alcohol with cefotetan/cefazolin Low gram coverage IV: renal dysfunction , allergy to cephalosporins or PCNs NR: “Cef-” or “Ceph-”
Aminoglycosides Vancomycin Gentamicin* Bactericidal- binds to cell wall and inhibits peptidoglycan synthesis Protein synthesis inhibitor Gram+ ONLY DOC- MRSA ; serious Staph in pts allergic to Beta-lactams; C. Difficile (oral; localized effect. Not absorbed orally ) Serious Gram-; Gram+ for synergy ONLY Red Man’s Syndrome (flushing, rash, pruritis, urticaria, tachycardia, hypotension) ; nephrotoxicity, ototoxicity, phlebitis Nephrotoxicity; ototoxicity (50% IRREVERSIBLE. Cochlear high tone hearing affected, vestibular dizziness, Avoid IM (pain, necrosis) Infuse of 60mins Measure levels to adjust dose (trough) Complete course Note exact time of admin and when levels drawn Monitor ototoxicity & nephrotoxicity Extended-interval
IV: Renal dysfunction DDIs: ototoxic & nephrotoxic drugs; skeletal muscle relaxants; PCNs IV: renal dysfunction headache, vertigo, tinnitus); AG-induced NM blockade dosing (^) Decreases risk of nephrotoxicity. Get trough levels only (goal: <1mg/dL) Trough: just before next dose Peak: 30mins after 30min infusion