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H1 ANTIHISTAMINES
Found in vascular smooth muscle, bronchi, and sensory nerves
Often combined with adrenergic drugs to offset each others side effects
Compete for receptors but don’t have ability to bump off endogenous histamine on receptor due to weak affinity
• Typical examples
o First Generation- older agents (more of an attraction for H1 receptors in CNS/brain making them more sedating)
▪ diphenhydramine (Benadryl)
• leading ingredient in sleep aids
▪ hydrOXYzine
▪ Others
o Second Generation- less sedating and less of an attraction for H1 receptors in CNS (tend to be attracted to H1 receptors in periphery)
▪ Cetirizine
• zyrtec
▪ loratadine
• allegra
▪ fexofenadine
• Claritin
• Mechanism of action
o Blocks the action of histamine at H1 receptors
• Indications
o Allergies, inflammation and pruritus
• Side effects
o Anti-cholinergic effects (inhibit action of Ach)
o Drying effects
o Sedation or paradoxical excitation (list as an allergy)
• Nursing Implications
o Monitor for sedation (particularly true in elderly- increases their risk of falls)
o Don’t use to put kids to sleep
▪ Can over-medicate and cause coma/death
• Patient Education
o Safety concerns
o Possible paradoxical excitation
• See slides of Antihistamines and Zyrtec
NSAIDs (Non-Steroidal Anti-inflammatory Drugs)
• Inhibits cyclooxygenase (COX) enzyme- helps to mediate immune responses
o COX 1- present in all tissues, associated w/ inflammation, reduces gastric acid production (GI upset), increases platelet aggregation, promotes vasodilation, dilates bronchi
▪ when inhibited we get opposite effects
o COX 2- produce prostaglandins which causes pain
Typical Examples
o Non-selective COX inhibitors- both pathways inhibited (Cox 1 & 2)
← ASA- acetasilic acid
← ibuprofen
o acetaminophen has no anti-inflammatory properties
← naproxen
← ketorolac
o Selective COX-2 inhibitors- more direct mechanism of action
← celecoxib (Celebrex)
• Mechanism of Action and Indications
o Aspirin
← Inhibits COX-1 and COX-2
← Antipyretic (lowers fever), anti-inflammatory, and analgesic
− Have to take larger doses to achieve these which can lead to many side effects
← Prevents platelet aggregation (more often used for this action)
− Patient’s take these to decrease risk of heart attack and stroke
o Ibuprofen (motrin) and others
← Prevent formation of prostaglandins
− stop pain
← Analgesic and anti-inflammatory
← Used as first line therapies when treating inflammatory conditions like rheumatoid arthritis
← Used to reduce fever
o Selective COX-2 inhibitors
← Inhibit only COX-2
← Don’t affect GI system and platelets bc they don’t affect COX-1
← Used a lot for orthopedic post-op patients
• Side effects
o Aspirin
← GI distress
• Why we have enteric coated (dissolves later so it doesn’t hurt stomach)
← Bleeding (due to affect on platelets)
← Salicylism
• Can cause tinitis (ringing in ears), hearing loss, and metabolic acidosis if overdose
o Ibuprofen and others
← Less GI or bleeding issues than ASA
← Better tolerated than aspirin
← If someone is taking anti-coagulents & NSAIDS, this increases bleeding risks
o COX-2 inhibitors
← Abd pain (GI stuff like bloating)
← Used short term for the most part
• Nursing Implications
o Bleeding risk- look for signs like black, tarry stools (blood in stool) or hidden blood
← Contraindicated in bleeding disorders (ulcerative colitis, peptic ulcer disease, etc.)
o Monitor for salicylate toxicity (tinitis)
o Evaluate if what we gave reduced fever, pain, etc.
o ASA not used in hospital or with kids (under age 19 bc of increased risk of rhye’s syndrome which can lead to multi-system organ failure)
← Exception: Baby ASA (81 mg) or 325 mg q day
• Taking low doses to prevent other things like heart attack or stroke
• Patient Education
o Teach parents not to use ASA (why?)
▪ Bc of risk of rhye’s syndrome
o Report ringing in ears or dark tarry/bloody stools esp. w/ higher doses of aspirin
o Don’t crush EC tablets
See Stool for Occult Blood cartoon, NSAID Gym cartoon, Aspirin Woman cartoon
GLUCOCORTICOIDS
• Mechanisms of action
o Suppresses action and release of histamine and prostaglandins
o Inhibits action of phagocytes
• Indications for use
o Severe/Chronic inflammatory processes
o Prevent organ transplant rejection
o Cancer
o Cerebral edema
o Endocrine disorders
• Typical examples (systemic)
o Short Acting
▪ cortisone
▪ hydrocortisone
• cortisol (stress hormone- stress reaction)
o Intermediate Acting- more common
▪ prednisone
▪ methylpredisone
o Long Acting
▪ betamethasone
• cerebral edema
▪ dexamethasone
• can be given IV
• Side Effects- many and varied bc these work on many different cells/can affect many different body systems
o C ataracts
o U lcers and GI bleeding
o S kin: strae, thinning, bruising
▪ Long term use in elderly thins skin and makes skin extremely fragile to injury
▪ Can lead to really bad skin tears
o H ypertension/ Hirsutism
o I nfection
▪ Can mask usual signs and symptoms of infection bc these are quieting everything down
▪ Simple infection can grow quick and fast
o N ecrosis of femoral head
o G lycosuria
o O besity, Osteoporosis
o I mmunosuppression
▪ Suppress immune system to prevent rejection of new organ transplant
o D iabetes
• Nursing Implications
o Look for long term use
o Give in morning with food
▪ Natural pattern is to rise in the morning
▪ w/ food decreases GI upset
o Assess for S/Sx of infection due to immunosuppression and lack of traditional inflammatory reaction
o Teach patient how to avoid infections
▪ Stay away from kids and crowds of people
▪ Stay away from people who are sick
▪ Immunizations may be contraindicated esp. w/ live vaccine
• Might not have ability to mount reaction to vaccine
o Dose tapered prior to D/C
▪ Exogenous loading dose but tapers down so adrenal gland will wake up and do job again
▪ Don’t want to suddenly stop taking bc it can lead to sudden CVD collapse
o Intranasal and topical forms have less SE
▪ Bc they are not systemic
▪ Just taking care of problem where it occurs
• Patient Teaching
o Take oral doses in the morning with food
o Infection may be masked
o Report black tarry stools/”coffee ground” emesis
▪ Red blood cells reacted w/ HCl ( indicates GI bleeding
o Take exactly as prescribed
• See Corticosteroids cartoon (The Good, The Bad, and the Ugly)
ANTIPYRETICS
▪ Typical example
o Acetaminophen
▪ Now used post-surgery because it can decrease the need for narcotic pain medication
• Opioid epidemic in the US due to healthcare
▪ Comes in IV form now
o ibuprofen (see NSAID section)
• Mechanism of action
o Direct action at hypothalamus
▪ Works at direct level of hypothalamus by overriding pyrogens wanting hypothalamus to increase set point ( allows for vasodilation and dissipation of heat
o Peripheral dilation (sweating)
• Indications
o Fever and pain
o No anti-inflammatory properties
• Side effects
o Potential liver damage
▪ Doesn’t cause GI problems NSAIDS do
• Nursing Implications
o T > 100, look for prn order on MAR
▪ If prn is only for temp, only give for temp, not headache or anything else
▪ Document: why you gave it, when, and if it worked
o Contraindicated with liver disease
• Patient Education
o Maximum 4 grams per day from all sources
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