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Pharm Unit 2
Special concepts r/t Antimicrobials• Selective toxicity
– Ability to target without harming host• Susceptibility• Prophylaxis
– Neutropenia, Surgery, Endocarditis• Combination Therapy• Misuse – non-specific fevers, viruses
Resistance
Ch. 86
Aminoglycosides: Background• Resistance is beginning to limit use
– Gentamicin – cheaper but commonly used
– 20 diff aminoglycoside-inactivating enzymes– Reserve amikacin
• Bactericidal– concentration dependent– Post-antibiotic effect – several hours (prolonged)– NOT effective against anaerobes
Gentamicin (Garamycin)
MOA/ Use Narrow spectrum for gram negative bacilli- especially pseudo. Aerugenosa, E. coli, Klebs, Serratia
ADME Poor CSF Not absorbed orally Toxicity with wound irrigation Binds tightly to renal tissue Excretion primarily renal Dosage varies widely (.5 mg/kg to 25 mg/kg)
Adverse Effects Ototoxic R/t excess trough levels- sensory hairs HA, N, vertigo then high- pitched tinnitus (action?) Vestibules of ears and absorbs into tissues to kidney Nephrotoxic Total cumulative dose ATN (acute tubular necrosis- leads to renal failure) -- proteinuria, casts
(slough or big particles), increased BUN, increased Creatinine Elderly and children at risk Neuromuscular blockade Flaccid, weak muscles Dosage based Neurotoxic with peripheral muscles Hypersenditivity & blood dyscrasias (rare)
D = D – PCNs, Cephs, Vanco used in combo– PCNs inactivate – schedule issue?– Ethacrynic Acid – ototoxicity– Other nephrotoxics– Skeletal Muscle relaxants
Aminoglycosides: Special concerns• Neomycin most nephrotoxic• Scheduling once daily – Safer?
– Post-antibiotic effect– Washout – esp. in vestibule and kidneys– Typically only measure trough – up to 1hr prior to next dose – level should be ?
Ch. 91 Antifungal Agents
Systemic mycotic infections
• Opportunistic (host is immunocompromised, malnourished, ill): candidiasis, aspergillosis, cryptococcosis, mucormycosis
• Nonopportunistic: sporotrichosis, blastomycosis, histoplasmosis, coccidioidomycosisSuperficial mycotic infections
• Candidiasis• Dermatophytes
Major Classes of Antifungals• Polyenes• Azoles• Pyrimidine analogs• Echinocandins
Amphotericin B (Fungizone)MOA/ TE – Broad spectrum antifungal agent binds to ergosterol component of
fungal cell wall and increases permeability. – DOC for most progressive, potentially fatal systemic mycoses
ADME – Highly toxic (sterols)– Poor GI absorption - SLOW IV USE ONLY– Poor CSF– Break down human sterols and bug sterols
Adverse effects – almost 100% - varying
– Phlebitis– Fever, chills, nausea – pre-treat w benadryl / acetaminophen– Nephrotoxicity – residual if 4 g/day, 1 L NS, Monitor q 3-4 days– Hypokalemia– Bone marrow suppression
DDD nephrotoxics - flucytosine
Itraconazole (Sporanox)MOA/ TE – Azole group of antifungal agents that inhibits sythesis of
ergosterol – fungistatic to treat histoplamosis, meningitis of cryptococcus neoformans & disseminated candidiasis
ADME – PO or IV– Food abs. capsules, ¯ abs. of suspension– Metabolized in liver– 40% excreted unchanged in urine
Adverse Effects – Common – N, V, and D, rash, HA, edema– Rare - Hepatic necrosis, transient cardiosuppression
DDD – Inhibits cytochrome P450 isozymes– Increases levels of warfarin, digoxin, sulfonylureas, cyclosporine,
quinidine and many other drugs– Acid reduces decrease drug levels
**if system is impaired, drug levels will rise (cytochrome P450 isozymes)
Azoles: Special Considerations• Fluconazole [Diflucan]
– Lower toxicity level– Can be taken orally– SJS syndrome (Stephen Johnson syndrome)
• Ketoconazole [Nizoral]– Effect on sex hormones – inhibits production
Drugs for Superficial Mycoses• Dermatophytic infections (e.g., ringworm)
– Tinea pedis, tinea corporis, t. cruris, & t. capitis• Drugs
– Clotrimazole (Gyne-Lotrimin) – DOC for topical dermatophytic and candida infections of skin, mouth, vagina
• Vulvovaginal candidiasis– Griseofulvin (Grifulvin) - oral
• onychomycosis
Griseofulvin (Grifulvin V)MOA/ TE Superficial mycoses only – inhibits fungal mitosis – incorporates into keratin
Adverse Effects – Transient headache, rash, GI– Contraindicated in hepatocellular disease
DDD – Decreases warfarin
Ch. 92 Drugs fro Non-HIV Viral Infections
Viral Infections• Dilemma• Types
– HSV (Herpes-simplex)• Genitalia, mouth, face (HSV-2)• More sensitive to antivirals, less resistant
– VZV (Varicella Zoster)• Chicken pox – Shingles• Moderate sensitive
– CMV (Cytomegalovirus)• Less sensitive and more resistant
Acyclovir (Zovirax)MOA/ TE Suppress synthesis of viral DNA and is useful in treating HSV1,2 & VZV – no
cure
Adverse Effects – Intravenous: reversible nephrotoxicity, phlebitis• Infuse slowly – hydration – during & 2 hr after
– Oral: GI, vertigo– Topical: stinging
Nursing Implications – Resistance – type of clients– IV indicated for oral lesions in – STI control– Treatment for VZV in elderly and children (w/in 24 hr)– ONLY give po (low availability), topically or IV
– NO IV bolus, NO IM, or NO SubQ injections– Valacyclovir [Valtrex] – prodrug that increases oral
bioavailability by 55%– Without regard to meals
*check to see if admin is correct in bookBolus- def.
Ganciclovir (Cytovene, Vitrasert)MOA/ TE – Suppresses replication of viral DNA to treat CMV retinitis of
immune compromised clients & prevent CMV in transplant patients
Adverse Effects – Granulocytopenia & thrombocytopenia – Mutagenesis, carcinogenesis– Teratogenisis and infertility – (90d following cessation)
Valganciclovir (Valcyte) – prodrug for oral use
– Take intact – with food
Hepatitis C (HCV)• Transmission—blood and semen• Typically asymptomatic • Leading cause for liver transplants• Among most common causes of liver cancer• Not curable, only suppressible• Drugs
– Pegylated interferon alfa combined with ribavirin
Interferon alfa (Peg-Intron) Immune modulatory, antineoplastic, antiviralMOA/ TE – Blocks entry of virus, synthesis of viral m-RNA and proteins,
and viral assembly. Tx of chronic Hep B & C
ADME – Pegylated - makes drug longer acting– Only parenterally (SubQ)
Adverse Effects – Flu-like (fever, myalgia, HA, fatigue) & depression– Long/High dose – thyroid dysfunction, heart damage, bone
marrow suppression– Alopecia, GI, injection site pain, bruising
Ribavirin (Rebetol)MOA unclear – Used with Interferon A - together are DOC for
Hep C (HCV). – Therapy 24 to 48 weeks. Goal is SVR – sustained
virologic response (loss of detectable viral RNA)
Adverse Effects – Hemolytic anemia (a lot of RBCs that are broken)– Teratogenic (Category X) – two forms of BC
Dosage Based on weight
Teratogenic Can kill fetus
Hepatitis B - HBV • Transmission—blood and semen• Drugs
– HBV vaccine – Interferon alfa-2b [PEG-Intron]– Lamivudine [Epivir-HBV]- already developing resistance– Adefovir [Hepsera]
• Duration of treatment and relapse
Flu Vaccines• 3 strains – selected by CDC, FDA, & WHO• Inactivated
– IM• Live attenuated – LAIV (Flumist) – 2003
– Intranasally – MUST BE FROZEN– Only ages 5-49
• Efficacy – Who should receive it?– 1-2 wks before exposure & lasts for 6 mo
• Adverse effects– Fever, malaise, myalgia– Guillain-Barré syndrome – Swine flu vac. 1976– LAIV – runny nose, HA, cough – rare GBS, anaphylaxis
• Precautions and contraindications– Acute febrile illness, hypersensitivity to eggs
• Who should NOT without MD approval?– Allergy to egg– Previous severe reaction– GBS– Moderate, severe illness w/ fever– Children under 6 months– LAIV not for: adults over 50, children under 5, pregnants, children or adolescents on long-term
ASA therapy, chronic heart, lung disease
Drugs for Influenza
Oseltamivir (Tamiflu)MOA/ TE inhibit viral replication of Inf A&B and is used to prevent and treat same –
effective if implemented within 2 days of sxms
Adverse Effects – N&V– Confusion, self injury
Expensive Must be started prior to 48 hr
ATI p. 220 Ch. 32 Antidepressants
General Points• Most common psychiatric disorder• Major treatment method - medications
– Five major groups• Goal? • Sxms
– Depressed mood, loss of pleasure / interest in all or nearly all of one’s usual activities• Under-treated • More prevalent in women• Suicidal thoughts may increase w Rx
Tricyclic Antidepressants (TCAs)Imipramine (Tofranil)MOA/ TE/ Use – Blocks reuptake of the MAO transmitters NE (norepinephrine)
and serotonin. Elevates mood, thereby treating depression.– Other uses: bipolar disorder, neuropathic pain, insomnia,
fibromyalgia, OCD
Adverse Effects – Orthostatic hypotension, sedation, anticholinergic effects, diaphoresis, cardiotoxicity, seizures, hypomania, “yawngasm”- orgasm that occurs when they yawn
Glands (Table 14-1) Salivary glands- decreased secretionSweat glands- decreased secretionBronchial glands-
Precautions/ Interactions – TCAs w MAOI can lead to severe HTN– Potentiates drugs like NE (norepinephrine)– Potentiate CNS depressants
Antidote – Activated charcoal after gavageDosing – Based on clinical response – don’t give more than a week
supplys– Dose at bedtime once levels achieved – EXCEPT in elderly
(cardiac reasons)
SSRI AntidepressantsFluoxetine (Prozac)
MOA/ TE/ Use – Selective serotonin re-uptake inhibitor resulting in elevated
serotonin levels – elevating mood and relieving depression.– Helps in bulimia nervosa
Adverse Effects – Impotence, weight gain, Serotonin syndrome, withdrawal syndrome, EPS, bruxism (clenching teeth and jaw), bleeding, hyponatremia.
– Some people have w/draw symptoms with this
Interactions MAOIs, Warfarin, & TCAs
MAOI AntidepressantsPhenelzine (Nardil)MOA/ TE/ Use – Enzyme – deactivates NE, serotonin, dopamine, and tyramine
(NE stimulator) from foods– NOT 1st CHOICE– Relevant P-kinetics
• Tyramine
Adverse Effects – CNS stimulation – agitation – hypomania – mania – hypotension – HTN crisis – meperidine (hyperpyrexia)
Deactivates tyramine which deactivates the transmitter
Atypical AntidepressantsBupropion (Wellbutrin)MOA Action unclear
Effect Stimulant ergo no wt gain No sexual dysfunction – may augment
Adverse Effects agitation, HA, dry mouth, constipation, wt loss, insomnia, tachycardia, seizure
Note St. John’s Wort (Box 32-2)
Other
(ATI p. 203 or 220??)
Used in smoking cessation Known to bring on seizures Can enhance sexual functions Consider this a vitamin (herbal supplement) May have an impact with BCP
Ch. 34 Classification: Sedative- Hypnotics
Overview• Venacular
– Anti-anxiety, anti-anxiolytics, tranquilizers– Hypnotics
• Major Categories – Benzodiazepines, Barbiturates, Barbiturate–Like– Miscellaneous
• Major Effects– CNS depression
• Therapeutic Uses– Relieve anxiety, facilitate sleep, manage muscle spasms, seizure and panic disorders, augment
anesthesia, and manage ETOH withdrawal
Benzodiazepines (CIV) Category DDiazepan (Valium) – self limiting
Others: clonazepam, lorazepam, clorazepateMOA – Depress neuronal function at multiple CNS sites by potentiating
endogenous GABA (gamma-aminobutyric acid) and is limited because GABA is finite®safer
Cardiac PO effect - heart & blood vessels (not a huge effect) IV effect – potentially ? (huge effect)
Respiratory Minimal alone, serious if combo or IV
Pharmacokinetics – Readily absorbed – Differ in respect to time - course of action
• (main indicator for which one chosen for which job)
Adverse Effects CNS – daytime vs. nighttime impacts– Amnesia– Paradoxical- opposite effect– Abuse– Malnutrition, liver disease and blood levels
DDD w/ other CNS depressants
Dosage varies by agent
Low Albumin Low circulation of drug (malnutrition)Nursing Implications ATI p. 218
Benzodiazapine-likesZolpidem (Ambien) CIVMOA/ TE/ Use – Agonists at benzodiazepine receptor
site on GABA channel prolonging sleep duration and helps relieve insomnia
– Low potential for tolerance or abuse
Adverse Effects Causes sleep walking, or not safe effects for the person
– Similar to benzodiazepines (daytime drowsiness / dizziness)
– Can intensify CNS depressants
Dosage/ Administration Before bedtime?- about 1 hr before bedtime
Melatonin AgonistRamelteon (Rozerem)MOA/ TE/ Use Activates melatonin receptors and rapidly induces
sleep to treat insomnia
Adverse Effects Somnolence, dizziness, and fatigue, reduced libido
Precautions ETOH, liver impairment, dangerous activities
BarbituratesSecobarbital (Seconal)MOA/ TE/ Use Mimics GABA and depresses CNS directly causing
relaxation and anxiety reduction. Other uses: seizure management, anesthesia, sleep disorders, mania
ADME NO CEILING TO LIMITS OF CNS depression (mimics GABA)
Adverse Effects Resp. depression, hypotension in toxic doses, can readily cause death
Precautions – Highly addictive - physical dependence – withdrawal can be severe
– Caution in elderly– Caution with other CNS agents– Caution with IM injection
Ch. 37 Drug Abuse
Terms• Drug abuse- using a drug in a fashion inconsistent with medical or social norms• Addiction- a disease process characterized by the continued use of a specific psychoactive substance
despite physical, psychologic, or social harm• Cross-tolerance- is a state in which tolerance to one drug confers tolerance to another • Psychological dependence- an intense subjective need for a particular psychoactive drug• Physical dependence- a state in which an abstinence syndrome will occur if drug use is discontinued• Cross-dependence- refers to the ability of one drug to support physical dependence on another drug• Withdrawal syndrome- a constellation of signs and symptoms that occurs in physically dependent
individuals when they discontinue drug use
Table 37-1 Diagnostic Criteria for Substance Abuse and Dependence
Ch. 28 Classifications: Opioid (Narcotic) Analgesics, Opioid Antagonists, Non-opioid Centrally Acting Analgesics
Intro to Opioids• Chemical class: Opioid vs. opiate• Functional class: Narcotic Analgesic• MOA – body peptides (3) enkephalins, endorphins, dynorphins• Opioid receptors - mu, kappa, and delta
– Agonist, partial agonist, antagonist• Partial agonist- partially mimics, if give with drug can compete with another drug and
negate it or antagonize it--- produces low to moderate activation alone– Strong and moderate to strong
Table 28-1 Important Responses to Activation of Mu and Kappa Receptors
Opioid AgonistsSTRONG: Morphine (Duramorph) CIIMODERATE to STRONG: Codeine (Paveral) CIIIMOA/ TE – Mimics action of endogenous opioid receptors (mu) to produce
analgesia and thereby relieve pain– Other effects include drowsiness, mental clouding, anxiety reduction,
sense of well-being
Adverse Effects – Resp. depression• Diminished by “tolerance” • Most common cause of OD death
– Others • Constipation, orthostatic hypotension, urinary retention /
urgency, cough suppression, biliary colic, emesis (usually with codeine), elevated ICP (intracranial pressure), dysphoria, sedation, miosis, neurotixicity, immune and hormone suppression with prolonged use
– Toxicity • Classic triad (coma, resp. depression, pinpoint pupils)
DON’T USE Caution: don’t use morphine with head injuries – if there is pressure in the head, the vessels constrict
ADME (pharmacokinetics) Nursing Implications
– Given by several routes– Slowest to fastest– Time-frame for TE varies by mode of administration – Denatured in liver– Hard to cross blood-brain barrier
Precautions/ Contraindictions
– Decreased resp reserve, pregnancy, head injury, infants / elderly, hypotension, liver disease
Interactions – CNS depressants, antihistamines, antihypertensives, MOAIs*, antiemetics, amphetamines, agonist-antagonist, antagonists
Dosage Highly individualized (Table 28-5)Administration – po, IM, IV, SQ, topical
– Oral associated with chronic– Preferably fixed schedule– Site specific – hazards- epidural- effects delayed
Miosis- pinpoint eyes (constriction)
Mydriasis- linked to dialated eyes
Other strong opioidsFentanyl (Sublimaze) – Anesthesia primary use (injectable)
– 100 X mg potency of morphine– Commonly seen as transdermal
• No children under 2 / none for under 18 less than 100 lbs.
Transmucosal (popsicle) • Breakthrough cancer pain• Store carefully• very large amts of drug
Meperidine (Demerol) – Interacts with several drugs– Toxic metabolite
• Avoid use past 48 hrs and not to exceed 600mg/24hr.
Hydromorphone (Dilaudid)MethadoneHeroin Crosses blood-brain easier
Moderate to Strong Opioid AgonistsCodeine – Usual dose of 30 mg = about same relief as 325 mg
of ASA or Tylenol– Combo meds more effective– Extremely effective cough suppressant at 10 mg
dose range
Oxycodone (OxyContin) & CR formsHydrocodone (Lortab, Norco) CIIIProproxyphene (Darvon, Darvocet) CIV
Special Clinical Concepts r/t Use of Opioids• Pain assessment – including evaluation!• Dosing amt and schedule• Fear of addiction in clinical setting• Avoiding withdrawal – 20 days or more• Patient controlled anesthesia (PCA)• Morphine: DOC - heart attack (MI)• Meperidine [Demerol]: DOC OB in delivery• Avoid opioids in Head Injury…
Nursing Implications (ATI p. 133 or 150)
Class: Opioid Agonist- Antagonists (Partial agonist)Pentazocine (Talwin) Others: nalbuphine (Nubain), butorphanol (Stadol)MOA • act mostly at mu, kappa receptor to produce
analgesia and relieve pain– Alone = agonist action– With agonist = can antagonize (blocks
mu receptor)
Adverse effects Similar to opioidsADME (Pharmacokinetics) – Less respiratory depression, low abuse
potential– Less effective pain relief– *Can start withdrawal sxms in opioid
addiction
Class: Opioid AntagonistsNaloxone (Narcan)MOA/ TE/ Use – competes for opiate site and blocks effects of opioid agonists /
agonist-antagonists – no significant effect given alone – resulting in REVERSAL of narcotic
ADME – Rebound effect – if you give morphine and narcan- the narcan may wear off first
Adverse effects Acute withdrawalDosage/ Admin 0.4 mg IM, IV, SubQOthers Naltrexone (ReVia) ETOH/ Opioid abuse
Non-Opioid: Centrally Acting AnalgesicsTramadol (Ultram) Others: clonidine (Duraclon) – pain/ HTN
MOA/ TE/ Use – Analog of codeine – binds w mu receptor producing analgesia to relieve pain- also blocks re-uptake of norepi (fight or flight or increase BP)
ADME (Pharmacokinetics) – Minimal potential for dependence or resp depression
Adverse effects Rare – most common: sedation, dizziness, HA, dry mouth, constipation
Precautions Can intensify other CNS dep. – ABSOLUTELY avoid MAOIs
Ch. 77 Laxatives
Bulk-formingMethylcellulose, phyllium (Metamucil)MOA/ Use – Behave like dietary fiber – nonabsorbable – swell to form viscous
solution / gel and softening fecal mass and increasing transit.– Temp relief of constipation, diarrhea, irritable bowel, ostomies
Adverse effects Esophageal & intestinal obstruction if not enough fluid ® ?(If this, then?)
Can obstruct (build a brick) the gut and won’t move through, therefore causing surgeryEsophagus- if you don’t drink enough to get pill down it can cling to walls and get stuck causing tears
SurfactantsDocusate sodium (Colace)MOA/ Use – Lower surface tension of stool and softens by facilitating
penetration of water into the feces– Act on intestinal wall to inhibit fluid absorption and stimulate
secretion of water and electrolytes into the intestinal lumen.
ADME – Full glass of water– Sit upright for 30 min– Effectiveness dose related (min 200 mg/day)
Dosage 50-500 mg dailyAdverse reactions RareOther – Bring water to the stool to soften it
– Typically see someone getting 200+ mg/day– New EBP says that anything under 200 is not effective
StimulantsBisacodyl (Dulcolax), Senna (Senekot)MOA/ Legitimate Uses – Directly stimulate gut motility, increase secretion of water and
ions into intestine, and reduce water and electrolyte absorption.– Uses: Treatment of (1) opioid-induced constipation and (2) slow
transit constipation
Dosage • related to formulation administered– Take bisacodyl no sooner than 1 hour after ingesting milk or
antacids – do not crush
Adverse reactions bowel rupture can occur
Osmotics (Salt prototypes)Sodium phosphate (Fleet) & Magnesium saltsMOA/ Uses Non-absorbable and retains water in the colon
Adverse reaction – Dehydration, diarrhea and loss of water (more with salts than with glycol)
– Magnesium can accumulate to toxic levels in renal failure– Sodium can retain fluid – so…. Contraindicated in patients with
heart failure HTN and edema
Other • glycol (MiraLax) – fewer side effects / safer
Miscellaneous• Lactulose- sugar base
– Action / Uses• Poorly absorbed and cannot be digested – by product of breakdown results in osmotic
diuresis• Enhances excretion of ammonia in liver failure
– SEs – flatulence, cramping• Glycerin Suppository• Polyethylene Glycol-Electrolyte (GoLytely)
– Safe in dehydrated or electrolyte sensitive
Additional Nursing Implications• High risk patients
– Contraindicated in abdominal pain, nausea, cramps, regional enteritis, diverticulitis, ulcerative colitis, acute surgical abdomen, fecal impaction, bowel obstruction.
• Abuse• Castor oil (powerful stimulant – avoid at night – not to children) p. 908
Ch. 69 Antihistamines
Background• Histamines – (Predominantly H1)
– Endogenous – Vessel effects – Bronchi effects – Stomach effects – Greatest interest
• Allergic reactions (mild / anaphylaxis)• PUD
Histamine Release• Allergic response
– Requires IgE antibodies– Prior exposure to allergen
• Non-allergic – direct stimulation of cells– Some drugs, chemicals, radiocontrast media, plasma expanders - require no prior exposure– Cell injury
Physio/ Pharm Effects• H1 Stimulation
– Vasodilation (If this, then?)– Vessel wall cells contract (If this, then?)– Bronchoconstriction (If this, then?)– Itching & pain– Mucus secretion– CNS effect – cognition / memory / sleep
• H2 Stimulation– Secretion of gastric acid (If this, then?)
• H2 blocker, block secretion of acid
Allergies & Pharmacology• Mild Allergy
– Hay fever, urticaria, mild transfusion rx.– Sxms caused by ? TX?
• Severe– Anaphylactic shock (bronchocontriction, hypotension, & edema of glottis)– Sxms caused by? TX? (ch 17)
• Other Uses– Common cold – runny nose
Antihistamines: 1st GenerationH1 Antagonists (classic antihistamines)
– No single prototype • dyphenhydramine [Benadryl]
– Highly sedating
MOA – Blockers (1st Gen)• Selectively bind to histaminic receptors• Can also bind to nonhistaminic receptor (muscarinic)
TE – Vessels (If blocks histamine, then ?)– Capillaries (If blocks, then ?)– Sensory nerves (If, then) – itching relief– Mucous membranes (If, then)
• If you block mucous production, then you get dryness– CNS
• Therapeutic doses (If, then) - sedation• Overdose – stimulation, seizures – esp. in young
– Other: relieve N & V, motion sickness
Clinical uses – Mild allergies, seasonal rhinitis, acute urticaria, allergic conjunctivitis, mild transfusion reactions
– Some block muscarinic & H1 receptor sites – useful for motion sickness
• promethazine [Phenergan] and dimenhydrinate [Dramamine]
– Insomnia (diphenhydramine [Benadryl])
Adverse effects – CNS• Sedation = to excess ETOH (If this, then?)• Dizziness, lack of coordination, confusion• Paradoxical: insomnia, excitation, tremors, convulsions
– GI• N, V, Diarrhea / constipation, loss of appetite
– Anticholinergic effects (memorize)– Cardiac Dysrhythmias w some 2nd Gen.
• Torsades de pointes, V-fib • terfenadine [Seldane] & astemizole [Hismanal] (neither
one is on market anymore)• Contraindications – third trimester• Precautions: asthma (bronchoconstriction- spasms), children/elderly,
urinary retention, HTN, OA glaucoma, prostatic hypertrophy Dry mouth, throat, nasal passages, thickened secretions, (cautions?), urinary histiancy, constipation, palpitations
D D D – ETOH, barbs/benzos/ opioids
Toxiciy – Sxms similar to atropine poisoning (anticholinergic), hyperpyrexia (fever)
– Can lead to death in children via excitation, hallucinations, convulsion, coma, CV collapse, death.
– Tx: remove and support – may use charcoal followed with cathartics
Antihistamines: 2nd GenerationPrototypes Fexofenadine (Allegra) – ExpensiveMOA/ TE Antagonists of histamine to relieve sxms of allergic rhinitis and urticarias
ADME Do not readily cross B-B barrier therefore non-sedating w minimized anticholinergic SEs
Precautions ETOH, drowsiness, liver, kidneys
Ch. 75 Drugs for Treating Allergic Rhinitis, Coughs, Colds
Allergic RhinitisReview of Sxms Sneezing, itching, runny nose, congestion
Common- conjunctivitis, sinusitis, asthma• Commonly associated disorders• Seasonal vs. Perennial
• Outdoor vs. indoor
Antihistamines• First line - oral• Prophylaxis first• No use against cold• Adverse effects
– 1st gen - sedation, anticholinergic– 2nd gen - rare
Intranasal GlucocorticoidsFluticasone (Flonase)MOA/ Use – Predominantly local anti-inflammatory
– First line - Most effective against all sxms
Adverse effects – Drying, burning, or itching– Rare - sore throat, epistaxis and HA– Rare - systemic – adrenal suppression / slowed growth in children
Dose • Adults – 2 sprays of 50 mcg. once daily
Intranasal CromolynCromolyn (NasalCrom)MOA/ Use – Suppresses release of histamine
– Best suited for prophylaxis– May not see results for week or more
Adverse effects Negligible
Sympathomimetics (Decongestants)Phenylephrine (Neo-Synephrine)MOA/ Use – Topical - rapid and intense
– Oral - prolonged, moderate, systemic effects– Also used in sinusitis and colds
Adverse effects – Rebound congestion– CNS stimulation– Cardiovascular– Hemorrhagic stroke w/ phenylporpanolamine (not on market
anymore)– Abuse (pseudoephedrine and ephedrine)– Cocaine
Mimics the syntheseticsNasal sprays – 2 – 3 sprays every 4 hours needed – not to exceed 5 consecutive
days– Use temporarily– Don’t want tissues to become dependant on it
• Don’t want them to think they have to have it for tissues to function
AnticholinergicsIpratropium bromide (Atrovent)MOA/ Use – Blocks cholinergic receptors and inhibits secretions to relieve
rhinorrea in allergic rhinitis and asthma– No systemic effects
SEs Drying, irritation
Leukotriene AntagonistMontelukast (Singulair)MOA/ Use – Blocks binding of leukotrienes to receptors thereby relieving
nasal congestion
Adverse effects None significant
Treatment of Coughs
Antitussives• Antitussives (cough suppressants)
– Actions / use: elevate cough threshold in common cold and URTI• Opioid (codeine and hydrocodone) - best
– Dosage: codeine 10 to 20 mg up to 6 times daily• Nonopioid (dextromethorphan) - best
– Opioid derivative w/o euphoria or dependence– Can lead to mind-body dissociation equal to PCP
ExpectorantsGuaifenesin (Mucinex)MOA/ Use Increases flow of respiratory tract secretions
MucolyticsAcetlcysteine (Mucomyst)MOA/ Use Directly thins secretions
ADME Inhalation delivery
Adverse effects Can trigger bronchospasm
Other antidote for Tylenol
Colds• Drug regimen
– Symptomatic– Combination products
• Decongestants• Antitussives• Analgesics• Antihistamines - anticholinergic to suppress mucus• Caffeine
Ch. 17 Treatment of Severe Allergy
Adrenergic AgonistEpinephrineMOA/ Use – Direct receptor binding (a 1&2, b1&2) mimicing the sympathetic
nervous system • Also known as sympathomimetic & catecholamine
ADME – Broken down quickly in stomach & significant 1st pass effect (can’t take by mouth)
– Can’t cross blood-brain– Discolors (pink/brownish) as it degrades (If, then?)
TE – Vasoconstriction (most common use)• Hemostasis• Augments local anesthetic via vascontriction• Elevates blood pressure• Restores beating heart• Bronchodilates
– TOC for anaphylactic shock– Mydriasis (rare use)
Adverse effects – HTN, necrosis, bradycardia w/ HTN, tachycardia, tremor, chest pain, elevated blood sugar
D D D – MAOIs– TCAs– General anesthestics (myocardial effects)
Precautions – IV admin can cause potentially fatal effect – check concentrations!
– Insure patent and healthy IV site
EpiPen • Anaphylactic deaths– PCN, venoms & foods
• Device: EpiPen & EpiPen Jr.• Storage & Replacement
– Room temp – dark – do NOT refrigerate• Injection
– Dose dependant on weight• Duration
– Around 20 min and monitor for 6 hours• SEs- heart rate increase
Ch. 76 Selected Drugs for Peptic Ulcer Disease (PUD)
Histamine2 – Receptor AntagonistsCemetadine (Tagamet) First choice for gastric / duodenal ulcersMAO/ Use Promote healing through acid reduction
GERD, Aspiration Pneumonitis in obese & gyne prior to anesthesia
Adverse effects – Low incidence of gynecomastia, reduced libido, impotence, CNS depression / excitement, pneumonia
D D D – Inhibits hepatic drug metabolism – therefore?– Major Drugs of concern – warfarin, phenytoin, theophylline,
lidocaine
Table 76-1 (use for histamine and rest of outline)
Famotadine (Pepcid)• For heartburn, acid indigestion, sour stomach• Cut dose in renal compromise/ failure• No antiandrogenic effects• No effect on hepatic metabolism of other drugs
Proton Pump InhibitorsOmeprazole (Prilosec)MOA/ Uses • suppress secretion of gastric acid
– Irreversible - days - up to weeks after cessation– Superior to H2RAs
Adverse effects – HA, diarrhea, N & V– Long term may increase risk of CA
ADME give 30 min before meal – once daily
DDD, DDF – Reduced absorption of atazanavir, ketocanazole and itracanazole – NOT recommended concurrently with atazanavir
AntacidsMagnesium hydroxide/ Aluminum hydroxideMOA/ Uses • alkaline agents that neutralize acid & decrease destruction of gut wall
– And prophylactically to prevent aspiration pneumonia
ADME – Take regularly to promote healing– In PUD: 1 and 3 hr after each meal & at bedtime– Goal is gastric pH greater than 5
Adverse effects – Constipation (aluminum base) / Diarrhea (magnesium base)– Sodium “loading”– High levels in renal failure clients
DDD May interfere with absorption of other drugs