Pharmacology midterm 1142

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GCSC

drug

any chemical that can affect living processes

pharmacology

the study of drugs (chemicals) that alter functions of living organisms

effectiveness

the most important property a drug can have-it is the ability of a drug to elicit the response for which it was given.

selectivity

a truly safe drug is one that cannot produce harmful effects, no matter the dosage or the length of administration- the goal is for drugs to ba as safe as possible

pharmacokinetics & the 4 components

processes that determine how much of an administered dose gets to its sites of action. The impact of the body on drugs.

* Drug Absorption
* Drug Distribution
* Drug metabolism
* Drug Excretion

pharmacodynamics

The impact of drugs on the body once a drug has reached its site of action.

drug receptor

special chemicals in the body that most drugs interact with to produce effects.

agonists

a drug that interacts with a receptor and stimulates the action of that receptor.

antagonists

produce their effects by preventing receptor activation

therapeutic index

a measure of a drugs safety

drug-drug interaction

occurs whenever a patient takes two or more drugs.

adverse reaction

: is any noxious, unintended, and undesired effect that occurs at normal drug doses.

side effect

a nearly unavoidable secondary drug effect produced at therapeutic doses.

toxicity

an adverse drug reaction caused by excessive dosing

allergic reaction

an immune response. There must be prior sensitization of the immune system for an allergic reaction to occur. Once it has, then re-exposure to that drug triggers and allergic reaction.

iatrogenic disease

a disease produced by a physician

organ specific toxicity

when drugs a toxic to certain organs

drug tolerance

decreased responsiveness to a drug as a result of repeated drug administration.

drug dependence

refers to a from habitual use of a drug, where negative physical withdrawal results from abrupt discontinuation.

placebo effect

the component of a drug response that is cause by psychologic factors and not by biochemical or physiologic properties of a drug.

therapeutic objective of drug therapy

"Provide Maximum Benefit, with Minimal Harm"

6 rights of drug administration

-Drug
-Route
-Dosage
-Time
-Patient
-Teaching regarding drug therapy

List, define and differentiate the 3 types of drug names

chemical name: constitutes a description of a drug using the nomenclature of chemistry.
generic name: assigned by the United States Adopted names Council, is also known as the proprietary name or the United States Adopted Name.
trade name: also known as the proprietary or trade name, are the names in which a drug is marketed

Discuss the clinical significance of plasma drug levels

Plasma drug levels are monitored to regulate drug responses.
If the levels are not at the desired numbers, then you can adjust the meds appropriately to achieve the desired response.

peripheral nervous system

Somatic Motor System- controls movement—especially the skeletal muscles

Autonomic Nervous System- controls many body processes and helps the body to maintain homeostasis.

parasympathetic functions

Slowing of heart rate
Increasing gastric secretions
Emptying of the bladder
Emptying of the bowel
Focusing the eye for near vision
Constricting the pupil
Contracting bronchial smooth muscle

Cholinergics

 Mimic the actions of the parasympathetic nervous system. They will either do the same things as the PNS or encourage these actions.
 Cholinergic- promote the action of the neurotransmitter, acetylcholine. [PARASYMPATHOMIMETIC]

cholinergics: principle structures affected by muscarinic activation

- Heart (slows HR)
- Exocrine glands-sweat glands, sebaceous glands, mammary glands, & glands that secrete digestive enzymes (increase secretions of these glands)
- Smooth muscles: (as follows)
• Lungs & GI Tract—contraction w/constriction of bronchi & increased tone & movement in GI muscles
• Bladder----contraction of some muscles & relaxation of others resulting in more effective emptying of the bladder & decrease in "bladder spasms"
• Vascular---relaxation w/ vasodilation (possible hypotension)
• Eye: Pupillary constriction (miosis) Contraction of the ciliary muscle resulting in accommodation (focusing of the eye by altering the curvature of the lens) for near vision. May see increased lacrimation (tearing)

cholinergics prototype drug

BETHANECOL (URECHOLINE)

cholinergics therapeutic uses

Uses-urinary retention (PRIMARY)

cholinergics secondary uses

GERD; paralytic (adynamic) ileus, gastric atony, & post-op abdominal distention when there is no gastric obstruction, or blockage, present

cholinergics adverse effects

- Cardiovascular: hypotension; bradycardia
- GI: excessive salivation, increased secretion of gastric acid , abdominal cramps, & diarrhea
- Urinary: contraindicated in patients with UT obrstaruction or weakness of the bladder wall
- Dysrhythmia in hyperthyroid patients: increased heart rate to the point of initiating an abnormal rhythm

cholinergics drug interactions

none of major concern

cholinergics administered

p.o. 1hr before or 2 hrs after meals (on an empty stomach). Adults 10-50mg 3-4 times a day

anti-cholinergics

Block the actions of the parasympathetic nervous system. These drugs will, mostly, do exactly the opposite of what the cholinergics do.

anti-cholinergics principle structures

- Heart (speeds rate & force of contraction)
- Exocrine glands-( decreases the secretion of these glands. Can even experience anhidrosis—absence of sweating
- Smooth muscles: (as follows)
• Lungs & GI tract-dilation and decreased tone & movement in GI muscles
• Bladder-urinary retention
• Vascular-vasoconstriction
• Eye-pupillary dilation (mydriasis); blurring of the vision; photophobia; decreased tearing.

Can't see
Can't pee
Can't spit
Can't poop

anti-cholinergics prototype drug

atropine

anti-cholinergics adverse effects

- Dry mouth
- Blurred vision, photophobia, elevated IOP
- Urinary retention
- Constipation
- Anhidrosis (absence of sweating)
- Tachycardia
- Asthma

anti-cholinergics drug interactions

- Antihistamines
- Phenothiazine antipsychotics
- Tricyclic antidepressants

anti-cholinergics adminstered

dosages vary---higher in emergency situations
- Oral
- IV
- IM( drawn up or pre-filled like AtroPen)
- Sub-Q
- Ophthalmic

Oxybutynin (Ditropan)

one other anti-cholinergic for overactive bladder

sympathetic

 Regulating the cardiovascular system
- Maintaining blood flow to the brain
- Redistributing blood flow during exercise
- Compensating for loss of blood through vasoconstriction
 Regulating body temp
- Maintaining blood flow to the skin
- Promoting production of sweat for cooling
- Promoting piloerection for warmth
 Implementing the "fight or flight" reaction
- Increasing HR and blood pressure
- Shunting blood from the skin & viscera into the skeletal muscles
- Dilating the bronchi to improve oxygenation
- Dilating the pupils to enhance visual acuity
- Mobilizing stored energy providing glucose for the brain and fatty acids for muscles

adrenergic agonists

mimic the actions of the sympathetic nervous system (sympathomimetic). The 2 classes of drugs considered to be adrenergic agonists are the catecholamines and non-catecholamines.

catecholamines

1) Cannot be used orally
2) Have a very brief duration of action &
3) Cannot cross the blood-brain barrier

Administered primarily IV push and/or through continuous IV infusion. Must be discarded if IV solution becomes discolored.

non-catecholamines

1) Can be given orally
2) Have a much longer half life than catecholamines
3) Less polar than catecholamines and more able to cross the blood-brain barrier

catecholamines examples

epinephrine, norepinephrine, isoproterenol, dopamine, & dobutamine.

non-catecholamines

ephedrine, phenylephrine, & terbutaline

adrenergic antagonists

cause direct blockade of adrenergic receptors. There are 2 major groups: 1) alpha blockers, and 2) beta blockers.

alpha blockers therapeutic uses

Essential hypertension
Reversal of toxicity from alpha-1 agonists
Benign prostatic hyperplasia
Pheochromocytoma
Raynaud's disease

alpha blockers adverse effects

Orthostatic hypotension
Reflex tachycardia
Nasal congestion
Inhibition of ejaculation

alpha blockers specific drugs

Prazosin (Minipress)-HTN
Terazosin (Hytrin)
Doxazosin (Cardura)-HTN
Tamsulosin (Flomax)-BPH
Alfuzosin (Uroxatral)
Phentolimine (Regitine)

beta blockers therapeutic uses

Angina Pectoris
Hypertension
Cardiac dysrhythmias
MI
Heart Failure
Hyperthyroidism
Migraine headache
Stage Fright
Pheochromocytoma
Glaucoma

beta blockers adverse effects

Beta-1:
Bradycardia
Reduced cardiac output
Precipitation of heart failure
AV Heart block
Rebound cardiac excitation
Beta-2:
Bronchoconstriction
Inhibition of glycogenolysis

beta blockers specific drugs

Propranolol (Inderal)
Atenolol (tenormin)
Metoprolol (Lopressor, Toprol)
Other beta blockers for cardiovascular disorders

central nervous system

➢ In the peripheral nervous system, only 3 compounds (acetylcholine, norepinephrine, and epinephrine) act as neurotransmitters, but in the CNS there are many compounds serving this function and probably many more that have yet to be discovered.
➢ We do not always know exactly how CNS drugs produce their effects.
➢ Since the CNS is essentially made up of the brain and spinal cord, the blood-brain barrier can be a very big issue with the action of CNS drugs. This barrier can both protect the CNS from toxic substances and block entry of medicines that might be helpful into the CNS.
➢ Some CNS drugs, such as psychotropic agents, may take 2-4 weeks to reach their maximum efficacy, and side effects that may be very pronounced in the beginning often will subside over time to a much more tolerable level. Tolerance, or decreased response to a drug over a prolonged period of use, and Physical dependence, or a state in which abrupt discontinuation of a drug would result in withdrawal symptoms—may also be issues with CNS drugs.

parkinson's disease

(PD) was first described in 1817 by Dr. James Parkinson, a British physician, for whom the disease was named. It is a disease that is characterized by four major features:

4 features of parkinson's disease

• Rest tremor of a limb (shaking with the limb at rest)
• Slowness of movement (bradykinesia)
• Rigidity (stiffness, increased resistance to passive movement) of the limbs or trunk
• Poor balance (postural instability)

anticholinergics

(trihexyphenidyl, benztropine mesylate, procyclidine, etc.) do not act directly on the dopaminergic system. Instead they decrease the activity of another neurotransmitter that controls movement, called acetylcholine, to balance out the production of dopamine and acetylcholine. In general, mild PD that consists of tremor at rest can often be treated initially with anticholinergic agents. Adverse effects of these drugs include blurred vision, dry mouth and urinary retention. Anticholinergics may be contraindicated in older patients because they can cause confusion and hallucination.
• The primary goal of medication therapy for Parkinson's for some time has been the reduction or slowing of symptoms.

dopamine agonists

• Classification: Dopaminergic drug (CNS—Anti-Parkinson's)
• Action: binds to dopamine receptors, improves motor performance, and reduce motor fluctuations.
• Adverse effects: hallucinations, daytime sleepiness, postural hypotension, nausea, dizziness, insomnia, constipation, weakness, dyskinesias, sleep attacks, and fetal injury.
• Drug interactions: Cimetidine, serotonin receptor agonists, and dopamine receptor antagonists.
• Contraindications: kidney dysfunction (pramipexole), pregnancy (ropinirole), use all dopamine agonists with caution in the elderly and patients with psychiatric disorders.
• Nursing Implications: assess bradykinesia, akinesia, postural instability, tremor, rigidity. Assess the extent to which they interfere with daily living activities. Start dosage low then gradually increase. Evaluate daily activity improvements as an ongoing evaluation. Involve the family for medication administration and improvements. Inform the patient regarding adverse effects and possibilities of minimizing these such as reducing nausea and vomiting by taking medication with food.
• Five dopamine agonists: Pramipexole (Mirapex), Ropinirole (Requip), Apomorphine (Apokyn), Bromocriptine (Parlodel), and Pergolide (Permax).

epilepsy

With seizures, a group of neurons in the brain will get really agitated or excited and decide to "cut up". The "electrical" discharges from this focus will frequently then travel to other areas of the brain—the severity of the seizure will be related to how much brain tissue or area is involved. Epileptic seizures can be caused by a variety of things, congenital defects, hypoxia at birth, head trauma, & cancer.

partial or focal

Seizures may be _______________ or ________ where a small amount of the brain may be affected resulting in much more limited seizure activity.

simple partial seizure

Discrete or localized symptoms related to the focal area of the brain affected. No loss of consciousness. May persist 20-60 seconds.

simple partial, complex partial and partial seizures that evolve to secondary generalized seizures (traditional drugs)

Carbamazepine Phenytoin Valproic acid Phenobarbital Primidone

simple partial, complex partial and partial seizures that evolve to secondary generalized seizures (newer drugs)

Oxcarbazepine, Gabapentin, Lamotrigine, Levetiracetam, Pregabalin, Topiramate, Zonisamide

complex partial seizures

Loss of consciousness; lack of responsiveness; staring with a fixed gaze; followed by a period of automatism during which the patient performs repetitive, purposeless movements, such as lip smacking. These seizures typically last 45-90 seconds.

partial seizures that evolve to secondary generalized seizures

Begin as simple or complex partial seizures and then evolve into generalized tonic-clonic seizures.

generalized seizures

Other seizures, affecting a much larger area of the brain are referred to as generalized and the nurse will see more in the way of convulsions. Generalized seizures may be categorized as follows:
tonic-clonic seizures (grand mal), absence (petit mal), myoclonic, atonic, status epilepticus, febrile seizures

tonic-clonic seizures (grand mal)

Major convulsions characterized by a period of rigidity (tonic phase) followed by a period of synchronous muscle jerks (clonic phase). Patients will generally be incontinent of urine

tonic-clonic seizures (grand mal) medications

traditional drugs: Carbamazepine Phenytoin Valproic acid Phenobarbital Primidone

Newer drugs: Lamotrigine Topiramate

absence (petit mal)

Loss of consciousness for about 10-30 seconds with or without mild symmetric motor activity. May occur many times a day & occur primarily in children subsiding generally by the teenage years.

absence (petit mal) medications

traditional drugs: Ethosuximide Valproic acid

Newer drugs: Lamotrigine

Myoclonic seizures

Sudden muscle contractions either focal myoclonus, with seizure activity involving just one limb, or massive myoclonus involving the muscles of the whole body. Last for about 1 second.

myoclonic seizures medications

traditional drugs: Valproic acid

Newer drugs: Topiramate

atonic seizures

Sudden loss of muscle tone-may be related only to the muscles of the head and neck, resulting in "head drop", or the muscles of the trunk and limbs, resulting in a "drop attack" or sudden collapse of the patient. Occur mainly in children.

atonic seizures medication

traditional drugs: Valproic acid given with benzodiazepines

newer drugs: Possibly Valproic acid in combination with lamotrigine

status epilepticus seizures

Seizures persisting for 30 minute or longer

status epilepticus seizures medications

traditional drugs: Valium (Diazepam); Ativan Lorazepam) given IV

newer drugs: May also try high dose AED's

febrile seizures

Associated with high fever usually in children from 6 months to 5 years of age—tonic-clonic seizures usually of short duration. This is not nor does it lead to epilepsy.

febrile seizures medications

traditional drugs: Control the fever and prevent aspiration—if need be treat with Valium, Ativan as ordered in age-appropriate doses.

newer drugs: N/A

anti-epileptic drugs (dilantin)

Generic name: Phenytoin
Trade name: Dilantin, Phenytek
Classification: Antiepileptic
Action: selective inhibition of sodium channels, stabilizes neuronal membranes, and limits the spread of seizure activity by affecting the motor cortex.
Adverse effects: gingival hyperplasia, nystagmus, morbilliform rash, effects in pregnancy, dysrhythmias, hypotension, and hirsutism.
Drug interactions: decrease effectiveness of oral contraceptives, warfarin, and glucocorticoids. Diazepam, isoniazid, cimetidine, alcohol, carbamazepine, phenobarbital, and barbiturates should be avoided.
Contraindications: sinus bradycardia, sinoatrial block, second or third degree atrioventricular block, or Stokes-Adams syndrome. Pregnancy can be a contraindication also unless the benefits of the seizure control outweigh the risk to the fetus.
Nursing Implications: Assess for the type of seizure involved and the frequency of the seizures. Perform periodic blood studies for therapeutic levels. Check hepatic and renal functions. Advise patient to avoid hazardous activities such as driving until seizure control has been achieved. Advise patient to carry a Medic Alert bracelet for proper emergency treatment. Teach patient and a family member to maintain a seizure frequency chart. Instruct patient to take medication exactly as prescribed, educate on possible side/adverse effects, warn patients against use of depressants such as alcohol, encourage routine dental care, warn patients against abrupt cessation of treatment, and instruct patient to take medication with meals.

anti-epileptic drugs (phenobarbital)

Generic name: Phenobarbital
Classification: Antiepileptic (also anticonvulsant barbiturate)
Action: binds to GABA receptors, causing the receptor to respond more intensely to GABA itself.
Adverse effects: lethargy; depression; learning impairment; irritable and hyperactive (children); agitation and confusion (elderly); physical dependence; exacerbation of intermittent porphyria; rickets and osteomalacia.
Drug interactions: oral contraceptives, warfarin, alcohol, benzodiazepines, opioids, and valproic acid.
Contraindications: history of acute intermittent porphyria and pregnancy.
Nursing Implications: Assess for the type of seizure involved and the frequency of the seizures. Administer IV slowly and monitor for excessive CNS depression when large doses are given. Advise patient to avoid dangerous activities such as driving due to possible sedation, advise to inform physician if children become irritable and hyperactive, warn women of child-bearing age of possible birth defects, warn patients against abrupt cessation of treatment, and warn patients against use of depressant such as alcohol. Advise patient to carry a Medic Alert bracelet for proper emergency treatment. Teach patient and a family member to maintain a seizure frequency chart. Instruct patient to take medication exactly as prescribed.

anti-epileptic drugs (tegretol)

Generic name: Carbamazepine
Trade name: Tegretol, Carbatrol, others
Classification: Antiepileptic
Action: suppresses high-frequency neuronal discharge in and around seizure foci and reduces synaptic reaction.
Adverse effects: nystagmus, blurred vision, diplopia, ataxia, vertigo, unsteadiness, headache, leucopenia, anemia, thrombocytopenia, birth defects, inhibition of renal excretion of water, morbilliform rash, photosensitivity reactions, Stevens-Johnson syndrome, and exfoliative dermatitis.
Drug interactions: oral contraceptives, warfarin, phenytoin, and phenobarbital.
Contraindications: history of bone marrow depression or adverse hematologic reactions to other drugs. Pregnancy can be a contraindication also unless the benefits of the seizure control outweigh the risk to the fetus. Use caution for patients with heart failure.
Nursing Implications: obtain complete blood counts prior to treatment. Know the type of seizure involved and the frequency of the seizures. Perform periodic monitoring of serum sodium content. Advise patient to take medication with meals, advise patient of the effects on other medications (such as oral contraceptives and warfarin), warn patients against abrupt cessation of treatment, and instruct the patient to avoid grapefruit juice. Advise patient to carry a Medic Alert bracelet for proper emergency treatment. Teach patient and a family member to maintain a seizure frequency chart. Instruct patient to take medication exactly as prescribed.

anti-epileptic drugs (depakote)

Generic name: Valproic acid
Trade name: Depakene, Depakote, Depacon
Classification: Antiepileptic
Action: suppresses high-frequency neuronal firing through blockade of sodium channels, suppresses calcium influx through T-type calcium channels, and it may augment the inhibitory influence of GABA.
Adverse effects: nausea, vomiting, indigestion, hepatotoxicity, pancreatitis, neural tube defects, rash, weight gain, hair loss, tremor, and blood dyscrasias.
Drug interactions: Phenobarbital and phenytoin.
Contraindications: significant hepatic dysfunction and for children under the age of three years who are taking other AEDs. Pregnancy can be a contraindication also unless the benefits of the seizure control outweigh the risk to the fetus.
Nursing Implications: Assess for the type of seizure involved and the frequency of the seizures. Use the lowest effective dosage, evaluate liver function at baseline and periodically, inform patients about sings and symptoms of liver injury (such as reduced appetite, jaundice etc) and to inform the physician. Advise patient to take with meals; instruct patient to swallow tablets/capsules whole; inform patient about signs of pancreatitis (such as abdominal pain, anorexia etc) and to seek immediate evaluation; warn patients against abrupt cessation of treatment and advise women of child-bearing age to use an effective form of birth control along with 5 mg of folic acid daily. Advise patient to carry a Medic Alert bracelet for proper emergency treatment. Teach patient and a family member to maintain a seizure frequency chart. Instruct patient to take medication exactly as prescribed.

anti-epileptic (neurontin)

Generic name: Gabapentin
Trade name: Neurontin
Classification: Antiepileptic; also used as adjunctive therapy to treat post-herpetic pain, and peripheral neuropathy pain
Action: unknown—does not directly affect GABA receptors—it may enhance GABA release, increasing GABA-mediated inhibition of neuronal firing.
Adverse effects: somnolence, dizziness, ataxia, fatigue, nystagmus, and peripheral edema.
Nursing Implications: Asses for the type of seizure involved and the frequency of the seizures. Assess renal functions and reduce dosage in patients with renal impairment. Advise patient to avoid driving and other dangerous activities until they are confident they are not impaired. Advise patient to carry a Medic Alert bracelet for proper emergency treatment. Teach patient and a family member to maintain a seizure frequency chart. Instruct patient to take medication exactly as prescribed

opioids (morphine)

Actions: Analgesia, anxiety reduction, euphoria, mental clouding, and drowsiness.

Therapeutic Use: The relief of pain

opioids (morphine) adverse effects

Respiratory depression, Constipation, Orthostatic hypotension, Urinary retention, Cough suppression (Codeine or hydrocodone) Biliary colic—spasms of the common bile duct with pain, Emesis, Elevation of Intracranial pressure. Euphoria/ Dysphoria, Sedation, Miosis
Neurotoxicity—delirium, agitation, myoclonus, & hyperalgesia because of renal impairment, cognitive impairment, or prolonged high doses of opioids
Tolerance
Physical dependence
Abuse issues (Controlled Substances Act)
Toxicity (overdose)—coma, respiratory depression, pinpoint pupils)

opioids (morphine) precautions

Decreased respiratory reserve
Pregnancy
Labor & Delivery
Head Injury
Infants, children, & the elderly
Inflammatory Bowel Disease
BPH
Liver disease

opioids (morphine) drug interactions

CNS depressants
Anticholinergic drugs
Anti-hypertensive drugs
Monoamine oxidase (MAO) inhibitors—Nardil, Marplan, & Parnate

opioids (other strong)

Fentanyl (Sublimaze)
Meperidine** (Demerol)
Methadone
Heroin
Hydromorphone (Dilaudid)

opioids (moderate to strong)

Codeine
Oxycodone (Oxycontin; Percodan)
Hydrocodone (Lortab; Vicodin)
Propoxyphene (Darvon; Darvocet)

agonist/antagonist opioids

Pentazocine (Talwin)
Butorphanol (Stadol)
Buprenorphine (Buprenex)
Nalbuphine (Nubain)

agonist/antagonist opioids side effects

**Low abuse potential; less respiratory depression; & less powerful analgesic effects. Should be given very cautiously, if at all, in patients who are physically dependent on a pure opioid agonist, like Morphine—can precipitate withdrawal symptoms.

Non-opioid centrally acting analgesics:

Tramadol (Ultram)

Narcotic antagonists:

Narcan—given IV to reverse actions of opioids. May require re-dosing in 1 hour or so. Revex does the same thing, generally does not require re-dosing.

Abortive therapy for migraine management

to stop an existing headache

Drugs for Migraine Headache:

NSAID's
Opioids
Ergotamine- the drug of choice for stopping ongoing migraine attacks; also used for cluster headaches

preventative (prophylactic) therapy

Beta blockers—Preferred drugs for migraine prevention (Inderal; Toprol)
Tricyclic antidepressants—Can prevent migraine and tension-type headaches; the underlying mechanism is unknown
Drugs used to treat epilepsy can reduce migraine attacks: divalproex (Depakote ER), topiramate (Topamax)
Estrogens (for menstrual migraine)
Other Drugs for Prophylaxis
Calcium channel blockers—Verapamil and flunarizine are the only two calcium channel blockers that appear useful in relieving migraines
Candesartan (Atacand)—Appears about as effective as more established therapies (beta blockers, divalproex, amitriptyline) and is much better-tolerated
Riboflavin (vitamin B2)—Can reduce the number and severity of migraine attacks, but benefits are modest and develop slowly

cluster headaches

Occur in a series or "cluster" of attacks; each attack lasts 15 minutes to 2 hours and is characterized by severe, throbbing, unilateral pain in the orbital-temporal area; primary therapy is directed at prophylaxis; effective agents include prednisone, lithium, and verapamil; if an attack occurs despite preventative therapy, it can be aborted with oxygen, sumatriptan, or an ergot preparation

1st generation NSAIDS (aspirin: ibuprofen; aleve)

Classification: antipyretics, nonopioid analgesics, salicylates
Therapeutic uses: Inflammatory disorders including: Rheumatoid arthritis, Osteoarthritis. Mild to moderate pain. Fever. Aspirin: Prophylaxis of transient ischemic attacks and MI.
Action: Produce analgesia and reduce inflammation and fever by inhibiting the production of prostaglandins. Inhibits COX-1 and COX-2
Adverse effects:tinnitus. GI BLEEDING, dyspepsia, epigastric distress, nausea, abdominal pain, anorexia, hepatotoxicity, vomiting. EXFOLIATIVE DERMATITIS, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS. Anemia, hemolysis, increased bleeding time.ALLERGIC REACTIONS INCLUDING ANAPHYLAXIS AND LARYNGEAL EDEMA.
Drug interactions: Aspirin may ↑ the risk of bleeding with warfarin, heparin, heparin-like agents, thrombolytic agents, ticlopidine, clopidogrel, abciximab, tirofiban, or eptifibatide, although these agents are frequently used safely in combination and in sequence.
Ibuprofen may negate the cardioprotective antiplatelet effects of low-dose aspirin.
Aspirin may ↑ risk of bleeding with cefoperazone, cefotetan, and valproic acid.
May ↑ activity of penicillins, phenytoin, methotrexate, valproic acid, oral hypoglycemic agents, and sulfonamides.
May ↓ beneficial effects of probenecid or sulfinpyrazone.
Corticosteroids may ↓ serum salicylate levels.
Urinary acidification ↑ reabsorption and may ↑ serum salicylate levels.
Alkalinization of the urine or the ingestion of large amounts of antacids ↑ excretion and ↓ serum salicylate levels.
May blunt the therapeutic response to diuretics, and antihypertensives.
↑ risk of GI irritation with NSAIDs.
↑ anticoagulant effect and bleeding risk when using aspirin with arnica, chamomile, clove, feverfew, garlic, ginger, ginkgo, Panax ginseng, and others.
Contraindications: Hypersensitivity to aspirin, tartrazine (FDC yellow dye #5), or other salicylates
Cross-sensitivity with other NSAIDs may exist (less with nonaspirin salicylates)
Bleeding disorders or thrombocytopenia (more important with aspirin)
Children or adolescents with viral infections (may increase the risk of Reye's syndrome)
Peri-operative pain from coronary artery bypass graft (CABG) surgery.
Nursing Implications: Patients who have asthma, allergies, and nasal polyps or who are allergic to tartrazine are at an increased risk for developing hypersensitivity reactions. Assess pain and limitation of movement; note type, location, and intensity before and at the peak after administration. Assess fever and note associated signs (diaphoresis, tachycardia, malaise, chills).

2nd generation NSAIDS (celebrex; mobic)

Classification: antirheumatics, nonsteroidal anti-inflammatory agents, COX-2 inhibitors
Therapeutic uses: Relief of signs and symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and juvenile rheumatoid arthritis.
Reduction of the number of adenomatous colorectal polyps in familial adenomatous polyposis (FAP), as an adjunct to usual care (endoscopic surveillance, surgery).
Management of acute pain and inflammation.
Action: Inhibits the enzyme COX-2. This enzyme is required for the synthesis of prostaglandins.
Has analgesic, anti-inflammatory, and antipyretic properties.
Adverse effects:Dizziness, headache, insomnia. edema. GI BLEEDING, abdominal pain, diarrhea, dyspepsia, flatulence, nausea. EXFOLIATIVE DERMATITIS, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, rash. Potential increased risk of Cardiovascular events and stroke.
Drug interactions: Significant interactions may occur when celecoxib is coadministered with other drugs that inhibit the CYP450 2C9 enzyme system.
May ↓ effectiveness of ACE inhibitors,thiazidediuretics, and furosemide.
Fluconazole ↑ celecoxib blood levels (dosage reduction recommended).
May ↑ risk of bleeding with warfarin.
May ↑ serum lithium levels.
Contraindications: Hypersensitivity
Cross-sensitivity may exist with other NSAIDs, including aspirin
History of allergic-type reactions to sulfonamides
History of asthma, urticaria, or allergic-type reactions to aspirin or other NSAIDs, including the aspirin triad (asthma, nasal polyps, and severe hypersensitivity reactions to aspirin)
Advanced renal disease
Peri-operative pain from coronary artery bypass graft (CABG) surgery
Should not be used in late pregnancy (may cause premature closure of the ductus arteriosus).Lactation: Potential for serious neonatal adverse effects. Discontinue drug or bottle feed.
Exercise Extreme Caution in history of ulcer disease or GI bleeding.
Nursing Implications: Assess range of motion, degree of swelling, and pain in affected joints before and periodically throughout therapy.
Assess patient for allergy to sulfonamides, aspirin, or NSAIDs. Patients with these allergies should not receive 2nd generation NSAIDS

acetaminophen/tylenol

Generic name: Acetaminophen
Trade name: Tylenol
Classification: antipyretics, nonopioid analgesics—DOES NOT HELP WITH INFLAMMATION
Therapeutic uses: Mild pain. Fever.
Action: Inhibits the synthesis of prostaglandins that may serve as mediators of pain and fever, primarily in the CNS
Adverse effects: GI: HEPATIC FAILURE, HEPATOTOXICITY(OVERDOSE). renal failure (high doses/chronic use). neutropenia, pancytopenia, leukopenia. rash, urticaria.
Drug interactions: Chronic high-dose acetaminophen (>2 g/day) may ↑ risk of bleeding with warfarin (PT should be monitored regularly and INR should not exceed 4).
Hepatotoxicity is additive with other hepatotoxic substances, including alcohol.
Concurrent use of sulfinpyrazone, isoniazid, rifampin, rifabutin, phenytoin, barbiturates, and carbamazepine may ↑ the risk of acetaminophen-induced liver damage (limit self-medication); these agents will also ↓ therapeutic effects of acetaminophen.
Concurrent NSAIDs ↑ the risk of adverse renal effects (avoid chronic concurrent use).
Propranolol ↓ metabolism and may ↑ effects.
May ↓ effects of lamotrigine and zidovudine.
Contraindications: Previous hypersensitivity, Products containing alcohol, aspartame, saccharin, sugar, or tartrazine
Nursing Implications: Assess overall health status and alcohol usage before administering acetaminophen. Patients who are malnourished or chronically abuse alcohol are at higher risk of developing hepatotoxicity with chronic use of usual doses of this drug. Assess amount, frequency, and type of drugs taken in patients self-medicating, especially with OTC drugs. Assess type, location, and intensity prior to and 30-60 min following administration. Assess fever; note presence of associated signs (diaphoresis, tachycardia, and malaise).

glucocorticoids and non-endocrine disorders (used to treat)

 Rheumatoid arthritis
 Systemic Lupus Erythematosis
 Inflammatory Bowel Disease
 Bursitis, Tendonitis, Gouty arthritis
 Osteoarthritis
 Allergic rhinitis
 Asthma
 Dermatological conditions
 Neoplasms in Acute Lymphocytic Leukemia, Hodgkin's and Non-Hodgkins lymphoma
 Suppression of Allograft Rejection
 Respiratory Distress Syndrome in Pre-Term Infants

glucocorticoids and non-endocrine disorders (adverse effects)

 Adrenal insufficiency
 Osteoporosis
 Increased risk for infection
 Glucose intolerance
 Myopathy
 Fluid & electrolyte disturbances
 Growth retardation in children
 Cataracts & glaucoma
 Peptic ulcer disease
 Iatrogenic Cushing's symptoms
 Rare psychological disturbances

glucocorticoids and non-endocrine disorders (drug interactions)

 Glucocorticoids increase urinary loss of K+, so use with caution in patients taking Digoxin, Thiazide, or Loop diuretics—monitor serum K+ levels
 NSAIDS—risk of GI ulceration
 Insulin & Oral Hypoglycemics
 Vaccines
**Contraindicated in patients with systemic fungal infections.

drugs for asthma

 Beta-2 Adrenergic Agonists—Protoype drug: Albuterol (Ventolin) & other "-olol" drugs
Review actions of these drugs from your Chapter 17 material (also on this handout)
 Glucocorticoids (as above)
 Methylxanthines—Prototype Drug—Theophylline (Aminophylline)
o Bronchodilator
o May be given IV or po
o Monitor serum drug levels

drug for asthma (adverse effects)

o Adverse effects: nausea, vomiting, diarrhea, insomnia, & restlessness—caffeine can intensify effects

drugs for asthma (drug interactions)

Phenobarbital, Dilantin, & Rifampin can lower serum levels of Theophylline
Tagamet, & fluoroquinolone antibiotics (like Levaquin) can increase levels of Theophylline

drugs for asthma (toxicity)

Overdose can cause severe cardiac dysrhythmias & convulsions

depression

The monoamine hypothesis of depression- depression is caused by a functional insufficiency of monoamine transmitters, norepinephrine (NE), serotonin, or both.

tricyclic antidepressants (TCA's) amitriptyline (elavil)

Intensify the effects of NE and serotonin by blocking the reuptake of them by the neurons.

amitriptyline (elavil) therapeutic uses

• Depression
• Bipolar disorder
• Neuropathy pain
• ADHD; OCD; & panic disorders

amitriptyline (elavil) adverse effects

• Orthostatic hypotension
• Anticholinergic effects ( can't see, can't pee, can't spit, can't poop)
• Sedation
• Cardiac toxicity
• Seizures
• Hypomania (mood is elevate too much)

amitriptyline (elavil) drug interactions

• MAO Inhibitors (Nardil, Marplan, & Parnate)
• Epinephrine/Norepinephin & Ephedrine or amphetamines
• Anticholinergics
• CNS depressants

amitriptyline (elavil) toxicity

***Huge issues with toxicity/ overdose---------cardiac dysrhythmias. These drugs can be tough to reverse.

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI's):

Uses: Depression
PROTOYPE DRUG: FLUOXETINE (PROZAC)

SSR's adverse effects

• Sexual dysfunction
• Weight gain
• Serotonin syndrome (most common when an SSRI is combined with a MAO Inhibitor—2-72 hours after initiation of treatment—altered mental status, agitation, confusion, disorientation, anxiety, hallucinations)
• Withdrawal syndrome
• Extrapyramidal symptoms (EPS)

SSR's drug interactions

• MAO inhibitors
• Warfarin (Coumadin)—may be displaced by Prozac
• TCA's & Lithium

SSR's prototype drug

PROTOYPE DRUG: FLUOXETINE (PROZAC)

other SSR's

have fewer sexual side effects
• Celexa
• Lexapro
• Paxol
• Zoloft

seratonin/norepinephrine reuptake inhibitors (s/nri's)

• Effexor
• Cymbalta

MAO inhibitors (MAOI's)

• Nardil
• Parnate
• Marplan

what choice are MAO's?

MAO's are 3rd & 4th choice antidepressant when TCA's & SSRI's have not worked. There are far too many side effects and drug/food interactions with these drugs to us willy-nilly.

sedative-hypnotic drugs

Benzodiazepines
PROTOTYPE DRUG: DIAZEPAM (VALIUM)

Benzodiazepines uses

• anxiety
• insomnia
• seizure disorders
• muscle spasms
• panic disorders
• assistance with induction of general anesthesia and/or conscious sedation
• withdrawal from alcohol addiction

Benzodiazepines adverse effects

• CNS depression
• Anterograde amnesia (impaired recall of events that take place after dosing)
• Paradoxical effects (occasionally have the reverse effect---insomnia, excitation, euphoria, etc)
• Respiratory depression (weak at this)
• Abuse
• Not to be used in pregnancy & lactation

Benzodiazepines drug interactions

• CNS depressants

**There can be big problems with tolerance, dependence, and overdoses with these drugs.

Benzodiazepine-like drugs

• Ambien/ Ambien CR
• Lunesta
• Sonata

barbiturates

CNS depressants & at hypnotic doses can have positive Cardiovascular effects.

barbiturates uses

• Daytime sedation
• Induction of sleep
• Seizure disorders
• Induction of general anesthesia and/or conscious sedation
• Treatment of insomnia

barbiturates adverse effects

• Profound respiratory depression
• Suicide
• Abuse (Tolerance & dependence)
• Hangover
• Not used in pregnant or lactating mothers

barbiturates drug interactions

• Other CNS depressants
• Warfarin (Coumadin)
• Oral contraceptives
• Phenytoin (Dilantin)

barbiturates (prototype drugs)

PENTOTHAL, SECONAL, PHENOBARBITAL

diuretics 4 types

• High-ceiling loop diuretics (Furosemide or Lasix)
• Thiazide diuretics (Hydrochlorothiazide or HCTZ)
• Potassium (K+) sparing diuretics (Spironolactone or Aldactone)
• Osmotic Diuretics

loop diuretics (lasix)

Block Na+ & Cl- reabsorption in the ascending limb of the Loop of Henle

lasix uses

• Edema
• Hypertension

lasix adverse effects

• Low Na+
• Low Cl-
• Low K+
• Dehydration
• Hypotension
• Rarely ototoxicity

lasix drug interactions

• Digoxin—if K+ level drops there is increased risk of cardiotoxicity
• Ototoxic drugs (such as gentamicin)

thiazide diuretics-hctz

Block reabsorption of Na+ & Cl- in the early segment of the distal convoluted tubule.

thiazide diuretics-hctz uses

• Essential hypertension-hypertension that develops with no apparent cause
• Edema
• Diabetes insipidus—actually helps to slow voluminous urine output

thiazide diuretics-hctz adverse effects

• Low Na+
• Low Cl-
• Low K+ (not as bad as Loop diuretics)
• Dehydration
• Hypotension
• Not used with pregnancy & lactating mothers

thiazide diuretics-hctz drug interactions

Essentially the same as the Loop diuretics
• Digoxin—if K+ level drops there is increased risk of cardiotoxicity

K+ sparing diuretics (Aldactone)

Promotes sodium excretion and K+ retention.

K+ sparing diuretics (Aldactone) uses

• Hypertension
• Edema

K+ sparing diuretics (Aldactone) adverse effects

• Elevated K+ levels
• ????Possibly a link to some benign and malignant tumors in lab rats????
• Endocrine effects (Aldactone is a mineralcorticoid—with hormone-like effects)

K+ sparing diuretics (Aldactone) drug interactions

• K+ supplements
• Salt substitutes (K+ Iodide)

other diuretics (mannitol)

Creates an osmotic force within the nephron to inhibit passive reabsorption of water.

other diuretics (mannitol) uses

• Prophylaxis of renal failure
• Reduction of intracranial pressure (ICP) [head trauma w/ brain edema]
• Reduction of Intraocular Pressure (IOP) [glaucoma or injury to the eye]

Osmotic diuretics (Mannitol) adverse effects

• Edema—may precipitate CHF & Pulmonary Edema in cardiac patients

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