Final Exam Flashcards
1
Q
Levothyroxine (Synthroid, Levoxyl)
A
Given for the treatment of hypothyroidism -Synthetic T4; Identical to naturally occurring thyroid hormone
-Converted to T3
Pharmacokinetics
- Given PO & well absorbed in empty stomach (30-60 min. prior to breakfast) EMPTY STOMACH needed*
- IV form available
- Highly protein bound
- Once per day dosing
- Takes about 1 month to reach plateau
-Since thyroid hormone occurs naturally in the body, almost anyone can take levothyroxine.
ο Pregnancy Category A (SAFE in pregnancy). The drug does pass in breast milk but is considered safe to use.
Adverse Effects
-Thyrotoxicosis- too much T3 and T4 (thyroid storm)
-Osteoporosis
-Atrial fibrillation
Absorption decreased by:
- Calcium supplements
- Antacids
- ron
- Cholesterol binding agents
- Food – esp. important to avoid infant soy formula, cotton seed meal, walnuts and high fiber foods (decreases absorption)
Drugs that accelerate metabolism of levothyroxine:
- Phenytoin, carbamazepine, rifampin
- Warfarin
- Levothyroxine accelerates the degradation of vit K dependent clotting factors
- There increased effects of warfarin
- Catecholamines
- Thryroid hormones increase the responsiveness to catecholamines…use cautiously
- Epinephrine, dopamine, dobutamine
- Insulin and digoxin
Levothyroxine can increase the requirements for both of these drugs
Nursing Implications:
- Monitor height and development in infants and children
- Teach to take on empty stomach
- Frequent follow up and lab monitoring
- Different brands of levothyroxine may NOT work the same
- Blood work after 6 weeks
2
Q
Methimazole (Tapazole)
A
Treatment for Hyperthyroidism
First line drug
MOA:
-Inhibits thyroid hormone synthesis
- Does not destroy existing stores of thyroid hormone
- Can take 3-12 weeks to achieve a euthyroid state
- Safer than PTU
- PO
Applications:
- Graves’ disease
- Adjunct to radiation therapy
- Suppress thyroid synthesis in preparation for thyroidectomy
- Avoid with pregnant women or breast feeding
Adverse Effects:
- Agranulocytosis most serious and dangerous toxicity- more prone to getting sick
- Dramatically reduces granuolcytes (type of WBC) needed to fight infection
Teach patient to Report sore throat, fever immediately!
3
Q
Propylthiouracil (PTU)
A
Indicated for hyperthyroidism
MOA: Decreases the synthesis of thyroid hormones
-Can also cause agranulocytosis
Different from Tapazole in that :-Causes severe liver injury
- Requires 2-3 doses per day
- Safer in pregnancy and in breast milk
- Blocks conversion of T4 to T3*
Indicated for:
- Pregnant women in 1st trimester
- breast-feeding women
- Pts with thyroid storm
- Pts intolerant of Tapazole
- Can treat at a higher dose with PTU than tapazole
4
Q
Beta Blockers and Hypothyroidism
A
ο Beta Blockers also have a role in treatment of hyperthyroidism. To help decrease the HR while we are waiting for the drug to treat the actual condition to kick in. For some people they stay on it at a low dose
ο Suppress tachycardia and other symptoms of Graves’ disease
ο Benefits derive from beta-adrenergic blockade, not from reducing levels of T3 or T4
- Also my be used in thyrotoxic crisis
- Contraindicated in pts with asthma*
Beta Blockers- OLOL
5
Q
Propranolol(Inderal)
A
Nonselectivebetaadrenergicantagonist (Beta1 andbeta2)
o ↓ HR, ↓force of ventricular contraction and slow impulse conduction through the AV node, suppress secretion ofrenin (Beta1)
o Bronchoconstriction (Beta2)
o Inhibits glycogenolysis (Beta2)
♣ Breakdown of glycogen to glucose
♣ Most detrimental to diabetics
o Lipid soluble – easily crosses membranes
o Well absorbed
o Widely distributed
o Hepatic metabolism
o Excreted in the urine
Drug interactions:
-Calcium channel blockers- decreases the calcium from allowing contraction so withbetablockers it decreases the force of the heart as well. So together it will make it even harder for the muscle to contract.Typicallynot prescribed together because can cause HF
-Insulin- more vigilant about screening for hypoglycemia
6
Q
Metoprolol(Lopressor)
A
Cardioselective(Beta1 only)- only impactsbeta1receptors.
Pt with emphysema can take this
Therapeutic Uses: o HTN, heartfailure andMI • Hepatic metabolism • Renal excretion • Adverse Effects o Bradycardia, ↓ CO, AV block, rebound tachycardia with abrupt discontinuation
7
Q
Local Anesthetics
A
Reversibly block all nerve impulses by disrupting permeability to sodium during action potential.
-Suppress impulse conduction along axons
- Conduction blocked only in neurons near the site of administration
- Sensations are blocked at different rates: pain first, followed by cold, warmth, touch, and deep pressure
-Not limited to sensory, may affect motor
Onset and duration affected by… Ð Molecular size Ð Lipid solubility Ð Degree of ionization Ð Regional blood flow- makes sure that the anesthetic gets good absorption
Frequently combined with epinephrine:
- Vasoconstrictor decreases local blood flow and delays systemic absorption of the anesthetic
- Decreases toxicity risk: less anesthetic used and slower absorption
Adverse Effects:
-Central Nervous System:
CNS agitation followed by depression
Cardiovascular system:
- Heart cause suppression of excitability
- Vessels causes vasodilation
Allergic reactions
-Varied
Labor and delivery
-Prolong labor by decreasing uterine contractility and maternal expulsion effort; can cause bradycardia and CNS depression in the neonate
8
Q
Lidocaine
A
- local anesthetic
- Administered topically and by injection
- Also used as an antidysrhythmic agent
- Duration of action depends on strength
- Addition of epinephrine
- Risk of systemic toxicity
9
Q
Lidocaine continued
A
Tetracaine is a topical lidocaine
- Surface anesthesia
- Pain, itching, soreness caused by infections, thermal burns, bruises, abrasions, plant poisonings, insect bites
Used in mucus membranes
-Risk for systemic toxicity
Systemic absorption determined by…
- Amount applied
- Skin condition
- Skin temperature
Administration:
- Smallest amount possible
- Avoid application to large areas
- Avoid application to broken skin
- Avoid strenuous exercise
- Avoid wrapping the site
- Avoid heating the site
10
Q
Injection
A
- Resuscitation equipment should be immediately available
- Maintain IV line for rapid treatment of toxicity
- Aspirate to ensure not administering in a vessel
11
Q
Infiltration Anesthesia
A
- Injected directly into area of surgery or manipulation
- If combined with epinephrine
- No end artery areas
- No fingers, toes, noses, ears, or penis
12
Q
Nerve Block
A
-Achieved by injecting a local anesthetic into or near nerves that supply the surgical field, but at a site distant from the field itself
-Local Anesthetics
Injection
13
Q
Intravenous Regional Anesthesia
A
-Used to anesthetize the extremities, but not the entire limb
-Anesthesia is obtained by injection into a distal vein of an arm or leg
-Tourniquet is applied to the limb to prevent anesthetic from entering the systemic –Local Anesthetics
Injection
14
Q
Epidural
A
- Achieved by injecting a local anesthetic into the epidural space
- Administration by bolus or by continuous infusion
- Diffusion blocks conduction in nerve roots and in the spinal cord itself
- Significant systemic absorption can occur
If given to pregnant mothers- Monitor for neonatal depression
15
Q
General Anesthetics
A
Analgesia and Anesthesia
- Analgesics are drugs that relieve pain without causing loss of consciousness.
- Anesthetics are drugs that produce unconsciousness & insensitivity to painful stimuli
- Produce unconsciousness and lack of responsiveness to all painful stimuli
- Inhalation agents
- Parenteral agents
16
Q
Balanced Anesthesia
A
Use of a combination of drugs to accomplish what we cannot achieve with an inhalation anesthetic alone
Compensates for lack of an ideal inhalation anesthetic
Allows for full general anesthesia at lower (safer) doses
General Anesthetics Inhalation Agents Minimal Alveolar Concentration -The amount of anesthetic inspired air must contain to produce anesthesia -Low MAC -High MAC
Inhalation Agents Uptake: -MAC -Pulmonary ventilation -Solubility of anesthetic in blood -Blood flow through the lungs
Distribution:
- Determined by regional blood flow
- Levels rise rapidly in brain, kidney, heart, and liver
Elimination
- Via lungs
- Anesthesia levels in the CNS decline more rapidly than in other tissues
Patients can waken from anesthesia before all anesthetic has left the body
17
Q
Adverse Effects of General Anesthesia
A
- Respiratory depression
- Cardiac depression- esp with someone who has cardiac issues
Increased risk with:
- Chronic respiratory problems
- Cardiac problems
- Significant obesity
Malignant hyperthermia
- Fatal reaction, genetic predisposition
- Muscle rigidity, T up to 43 degrees C
Treatment: dantrolene sodium
Aspiration of gastric contents
- Hepatotoxicity
- Toxicity to operating room personnel
- Headache, reduced alertness, spontaneous abortion
- Ensure proper venting of gases
18
Q
General Anesthetics
Inhalation Agents
A
Volatile liquids “–fluranes” EX: Isoflurane, enflurane, desflurane, sevoflurane -Rapid induction time -Easy to adjust -Rapid emergent time -Causes hypotension, bradycardia
Gases: Nitrous oxide
- “laughing gas”
- Adjunct in balanced anesthesia
- Can not produce surgical anesthesia alone
- *Powerful analgesic, weak anesthetic
19
Q
Adjuncts to in halation anesthesia ( pre-anesthesia/post anesthesia medications)
A
Pre-anesthetic meds: Benzodiazepines
- Reduce anxiety and promote amnesia
- Given to induce anesthesia or for conscious sedation
ex: Midazolam (Versed)
Opioids
-Pain relief, cough suppressant
Preanesthetic Medications
- Alpha 2-adrenergic agonists
- Anticholinergic agents
- Neuromuscular blocking agents
Postanesthetic Medications
- Analgesics
- Antiemetics
- Muscarinic Agonists
20
Q
Intravenous anesthetics
A
Propofol (Diprivan)
- Promotes release of GABA
- General CNS depression
- Induction and maintenance of GA
Sedation for mechanically ventilated patients, radiation therapy, diagnostic procedures
- IV administration
- Unconsciousness in less than 60 seconds
- Duration is 3-5 minutes
- Continuous infusion is needed for extended sedation
Adverse Effects
- Respiratory depression/apnea
- Hypotension
- Risk of bacterial infection
- Pain at the site of infusion
High abuse risk
21
Q
Opioids
A
MOA:
Opioid Receptors:
Mu and Kappa
Mu- opioids activate these
-Analgesia, respiratory depression, sedation, euphoria, physical dependence, and decreased GI motility
Kappa- opioids activate these
-Analgesia, sedations, and decreased GI motility
22
Q
Classifications of Opioids
A
- Pure opioid
- Agonist-antagonist opioid
- Pure opioid antagonist
23
Q
Morphine
A
Strong Opioid Analgesic
Schedule II- moderate to high abuse potential
Therapeutic Use:
- Analgesia
- More effective against dull pain, than sharp intermittent
- Post operative pain, cancer pain, labor and delivery pain
- Can be used for MI, dyspnea with heart failure
MOA:
binds to mu receptors
Adverse Effects:
- Respiratory depression
- Constipation
- Orthostatic hypotension
- Urinary retention
- Cough suppression
- Biliary colic- gallbladder attack- right upper quad. Pain. Blocked bile duct of the galbladder
- Emesis
- Elevated intracranial pressure- make sure their blood pressure is normal
- Euphoria/Dysphoria
- Sedation
- Miosis- more pupillary constriction
- Birth defects
- Neurotoxicity
Pharmacokinetics:
Routes of administration-
PO, IV, IM, SUB Q, Epidural, intrathecal- lower dose in the spine
-poor lipid solubility ( does not cross the blood brain barrier easily)
-inactivated by the liver and eliminated through the kidenys
TOlerance:
- With MSO4 tolerance develops to analgesia, euphoria, sedation, and respiratory depression. Tolerance typically only occurs with long term use or giving large loading doses or taking it more frequent then prescribed.
- Tolerance does not develop to constipation or miosis (pinpoint pupils)
- Cross tolerance exists among other opioid agonists- tolerance of different drugs in the same drug class
Physical Dependence:
- Abstinence syndrome when withdrawn
- Intensity of withdrawal parallels the degree of physical dependence
- DO NOT WITHDRAWAL ABRUPTLY
- Strong Opioid Analgesics
Precautions:
- Decreased respiratory reserve
- Labor and delivery
- Head injury- increase their ICP
- Old and young- hold on to drugs for longer. Watch doses.
- Liver impairment- will hold on to drug for longer.
Drug Interactions:
-other CNS depressants, anticholinergic drugs, hypotensive drugs, Mao inhibitors, opioids
Dosage guidelines:
- fixed schedule
- monitor vitals signs, especially respiratory rate
24
Q
Other Strong opioids
A
Fentanyl
- Parenteral
- Transdermal (Patch)
- Transmucosal
- Lozenge on a stick AKA Fentanyl pop- looks like candy. Beware of children
- Intranasal
Methadone
Hydromorphone
Meperidine
25
Moderate to strong Opioids
- Produce less analgesia and respiratory depression
- Produce sedation and euphoria
- Lower abuse potential
Adverse Effects- works on the same receptors
-Similar to MSO4
Examples:
Codeine
- 10% of the codeine dose is converted to MSO4 in the liver
- Some people lack the gene to metabolize codeine so it is ineffective
- Administered oral and parenterally
- Either alone or in combination with non-opioid analgesics (ASA or acetaminophen)
- Combination are effective because they relieve pain by different mechanisms
- Schedule II
- Combination products are Schedule III
- Only administered orally
- Effective cough suppressant
- *Nursing mothers should be alert for signs of infant toxicity such as excessive sleepiness, breathing difficulties, poor feeding---seek medical attention
Oxycodone, Oxycontin
- Oxycontin was reformulated in 2010 due to abuse
- New formulation bears the imprint OP the old formulation bears the imprint OC
- New formulation are harder to crush and if exposed to water or alcohol it turns into a gummy blob—cannot inject
Hydrocodone
-Combined with acetaminophen or ibuprofen
26
Agonist-antagonist Opioids
Pentazocaine
- Agonist at kappa receptors
- Antagonist at mu receptors
- Limited respiratory depression
Adverse effects similar to MSO4
-Can precipitate withdrawal in persons physically dependent on pure opioids
Buprenorphine
- Schedule III
- Partial agonist at mu receptors
- Antagonist at kappa
- Analgesic effects similar to MSO4
- Causes respiratory depression
- Can precipitate withdrawal in persons physically dependent on pure opioids
- Used in patients with severe chronic pain
- Solution for injection, transdermal patches, sublingual tablets, sublingual film
- Patches and solution for pain
- Sublingual products are used for opioid addiction
27
Using Opioids
- Pain assessment
- Prior to administration and I hour after and DOCUMENT pain scale
- VS- BP, HR, RR, o2 sat
What do we ask in a pain assessment????
- 0-10 sale
- Dosing
- Individual variation
Dosing schedule:
-Fixed
Specific Pain Treated with Opioids
- Postoperative
- Obstetrical
- Myocardial Infarction
- Head Injury
- Cancer Related Pain
- Chronic Noncancer Pain
Physical Dependence/Abuse/Addiction
- Physical Dependence
- Abstinence syndrome occurs if the dependence producing drug is abruptly withdrawn
Abuse
-Drug use inconsistent with medical or social norms
Addiction
- A disease process characterized by continued use of a psychoactive substance despite physical, psychological, or social harm
- Patient fears about addiction
28
Patient Controlled Analgesia-
typically morphine or fentanyl
- Self delivery of medication
- There is a ceiling to the amount they can receive even if they keep pressing the button
- Drug and dosages
- Patient and family education
29
Opioid Antagoinist
Naloxone (Narcan)
- Blocks opioid actions
- Will reverse effects of opioids if patient is receiving opioids
- Analgesia, respiratory depression, sedation, euphoria
- Can precipitate withdrawal in an opioid dependent patient
- d/t lingering effects you may have to push it again even after you revived them the first time
- Routes
- IV, IM, subQ, Nasal
30
Methylnaltrexone (Relistor)
Used for opioid induced constipation
-Selective mu receptors
Route:
-subQ
Adverse Effects
- Diarrhea
- Abdominal pain
- Flatulance
- Nausea
31
Non-opioid Centrally acting analgeiscs
Tramadol
- Weak activity at mu receptors
- Spinal inhibition of pain
- Used for mild to moderate pain
Clonidine
- Alpha 2 agonist
- Blocks nerve pathways that transmit pain in the spinal cord
- Used for severe cancer pain not relieved by opioids
32
Sedative-Hypnotic Drugs
- Drugs that depress central nervous system (CNS) function
- Primarily used to treat anxiety and insomnia
- Antianxiety agents or anxiolytics
- Distinction between antianxiety effects and hypnotic effects is often a matter of dosage
33
Sedative-hypnotics
Benzodiazepines
- Diazepam (Valium)
- Lorazepam (Ativan)* can give in IV form
- Midazolam (Versed)* Can give in IV form
- Alprazolam (Xanax)
Overview of pharmacologic effects:
- Central nervous system
- Reduce anxiety and promote sleep
- Cardiovascular system
- Oral vs. intravenous
- Respiratory system
- Weak respiratory depressants- be careful when mixing with opioids
Pharmacokinetics
- Absorption and distribution
- Readily cross the blood brain barrier
Metabolism
- Metabolites are pharmacologically active
- Time course of action
- Differ from one another in onset and duration and tendency to accumulate
Therapeutic uses:
- Anxiety
- Insomnia
- Seizure disorders
- Muscle spasm
- Alcohol withdrawal
- Perioperative applications
Adverse effects:
- CNS depression
- Anterograde amnesia- unable to make new memories
- Sleep driving
- Paradoxical effects
- Respiratory depression
- Great Abuse potiential
- Use in pregnancy and lactation
Other adverse effects
-hypotension
Drug interactions:
- other CNS depressants
Tolerance and physical dependence
- Tolerance
- With prolonged use, tolerance develops to some effects but not others
- Physical dependence
- Can cause physical dependence, but the incidence of substantial dependence is low
- Acute toxicity
Oral overdose: Drowsiness, lethargy, and confusion
Intravenous toxicity: Life-threatening reactions, profound hypotension, respiratory arrest, and cardiac arrest
General treatment measures
Oral: Gastric lavage, activated charcoal, saline cathartic, and dialysis
-Acute toxicity
-Antidote (Romazicon)
-Competitive benzodiazepine receptor antagonist
-Reverses the sedative effects of benzodiazepines but may not reverse respiratory depression
-Approved for benzodiazepine overdose and for reversing the effects of benzodiazepines after general anesthesia
-Routes of administration
-Oral
-Parenteral (intramuscular and intravenous)
34
Management of insomnia
Treatment is highly dependent on the cause
```
Non-drug therapy 1st
-avoiding naps
-decrease caffeine
-exercise (no later that 7p)
-environmet
therapy with hypnotic drugs
```
35
Drugs used for insomnia
- Benzodiazepines
- Benzodiazepine-like drugs: Zolpidem, zaleplon, and eszopiclone
- Ramelteon
- Antihistamines
36
Benzodiazapine like-drugs
Zolpidem [Ambien]
- Sedative-hypnotic
- Most widely used hypnotic
- Short-term management of insomnia
- Long term use: No apparent tolerance or increase in adverse effects
- Side effects: Daytime drowsiness and dizziness
Zaleplon [Sonata]
- Short-term management of insomnia
- Prolonged use does not appear to cause tolerance
- Most common side effects: Headache, nausea, drowsiness, dizziness, myalgia, and abdominal pain
Eszopiclone [Lunesta]
- For treatment of insomnia
- No limitation on how long it can be used
- Most common adverse effect: Bitter aftertaste
- Other common side effects: Headache, somnolence, dizziness, and dry mouth
37
Medications Affecting the Respiratory System
| Inhalation Medications
Enhances therapeutic effects
- Delivered directly to site of action
- Minimizes systemic effects
- Rapid relief of acute attacks
Delivery devices:
- Metered-dose inhalers
- Dry-powder inhalers
- Nebulizers
38
Metered-dose inhalers ( MDI)
inhaler has measured amount of drug with each puff. Need to shake it. Start to inhale with closed mouth on mouth piece.
Press and continue to inhale. Hold for 10 seconds. Take next dose if needed 1 to 2 minutes later.
MDI Spacers- you don’t lose med to atmospheric air. Good for kids that cant start inhaling before they press.
39
Dry powdered Inhaler
- many contain lactulose bulking agent helps raise medication- better facilitate med going in to the lungs
- You will not loose as much as you do in MDIs
- Pushing the lever back will get the med ready. Then pt will take good deep breath when ready. Pt. needs to be able to take a good breath to effectively get this medication.
- teaching re: lactose intolerance/allergies
40
Nebulizers
- liquid that sits in a canister. Add O2 or air to vaporize it and make it a mist that the pt. will inhale.
Typically 8 to 10 L of air needed.
Can be connected to mouth piece or mask.
In acute attack you would want to use this. Works better getting drug into the lungs (quicker). But you do not get the whole concentration all at once.
41
Classifications
Bronchodilators
- Adrenergics
- Anticholinergics
- Xanthines
Antiinflammatories
- Corticosteroids
- Leukotriene modifiers
- Mast Cell Stabilizers
```
Expectorants
Antitussives
Mucolytics
Nasal Decongestants
Antihistamines
```
42
Bronchodilators
Beta 2-Adrenergic Agonist
-Stimulate the Beta 2 adrenergic receptors in smooth muscle of bronchi and bronchioles
- Causes bronchodilation
- Relieves bronchospasm
- Suppresses histamine release in lung
- Increases ciliary motility- gets the mucus up
43
beta-2 adrenergic agonists
Short-acting beta 2 agonists (SABA)
-Taken PRN to relieve asthma attack- with exercise or you know you are going to be around a certain allergen.
EX: Albuterol (Proventil)
Long-acting beta 2 agonists (LABA)
- For patients that experience frequent attacks
- NOT PRN, taken on schedule
- ALWAYS combined with glucocorticoid- if you have COPD you can take LABA by itself- no glucocorticoid needed.
If patient has asthma and does not take glucocorticoid they can have asthmatic cardiac arrest.
EX: Salmeterol (Serevent Diskus)
The beta 2 adrenergic agonists are selective, they are not absolute
- Produce some activation of beta 1 receptors
- Results in tachycardia
- Monitor pulse before, during, after administration
CONTRAINDICATED: pts with angina, certain dysrhythmias
Other beta 2 effects: Tremor
44
Anticholinergics
Muscarinic Antagonist
Which Results in bronchodilation
- Approved only for COPD
- Off label use in asthma
Inhalation meds:
Ipratropium (Atrovent)
Tiotropium (Spiriva)
Ipatropium (Atrovent)
-Used for bronchospasm
Can be used in combination drugs:
-Combivent (ipratropium/albuterol)
AVOID with pts with PEANUT ALLERGY
Tiotropium (Spiriva)
-Long-acting
Maintenance therapy of bronchospasm
Adverse Effect: Dry Mouth
```
Xanthines
Mechanism of action is unknown
-Bronchodilation
-Inhibits pulmonary edema
-Increases ciliary action
-Decreases inflammation
```
Theophylline, Caffeine
- PO, Long-term treatment
- Toxicity: Activated charcoal
- N/V/D, insomnia, restlessness
- Lethal heart rhythms
Aminophylline IV infusion
-Administer slowly, rapid administration can cause hypotension and death
45
Anti-inflammatories
- Long-term control (daily dosing)
- Mainstay of asthma therapy
Corticosteroids (glucocorticoids):
First line treatment of asthma
- Airway inflammation is suppressed
- Decreases production of inflammatory mediators: leukotriene, histamine, prostaglandins
- Decreases infiltration of inflammatory cells (eosinophils, leukocytes)
- Decreases edema of airway
- Decrease mucous production
Restores or increases effectiveness of Beta 2 receptors
-Increases responsiveness to Beta 2 agonists
Inhalation:
- Fluticasone (Flovent)
- Mometasone (Asmanex)
PO:
-Prednisone
IV
-Methylprednisolone (Solu Medrol)
Nebulizer:
-Budesonide (Pulmicort Respules)
Adverse Effects:
- Oropharyngeal candidiasis
- Dysphonia (hoarseness, difficulty speaking)
Nursing action: Rinse and gargle after each administration
Teach importance of using spacer
46
Leukotriene Modifiers (antagonist)
Leukotriene’s (LT) are strong chemical mediators that cause bronchoconstriction, eosinophil infiltration, mucus production, airway edema
- Prevent LT from acting on target tissues
- Second line therapy, adjunct therapy
Singulair (montelukast) PO
- “I single out target cells”
Singulair indications:
- Prophylaxis and maintenance of therapy in asthma; NOT rapid relief of acute episodes.
- Prevent exercise-induced bronchospasm
- 2 hours before start of exercise/lasts approx. 12 hours
- Relief of allergic rhinitis
Adverse Effects
- Neuropsychiatric effects:
- Depression
- Suicidal thinking and behavior
47
Take home points re: respiratory mediations
- Albuterol is initial drug of choice for acute bronchospasm
- Aerosol products act directly on the airways = small doses=less side effects
- Anticholinergics most useful for long-term management of COPD
- Take inhaled corticosteroids on a regular schedule
48
Expectorants (coughing)
Liquefy respiratory secretions and allow for easier removal
Action= increases respiratory tract flow
Guaifenesin (Mucinex)
49
Mucolytics
Administered by inhalation or nebulized
- Liquefy mucus
- Productive cough
- Effective within 1 minute
Acetylcysteine (Mucomyst) Inhalation
-PO form used for acetaminophen overdose
50
Antipsychotic Agents
```
Used for broad spectrum of psychotic disorders:
¥ schizophrenia
¥ delusional disorders
¥ bipolar disorder
¥ depressive psychoses
¥ drug-induced psychoses
```
Other use: suppress emesis
51
Conventional antipsychotics~1st generation
Block receptors for dopamine in the CNS; cause extrapyramidal symptoms (EPS)- uncoordinated movements…
- May be classified by low potency (Thorazine), medium potency, or high potency (Haldol). Haldol has greater risk of EPS than Thorazine.
- Similar efficacy, difference in ability to produce side-effects (increased in high potency agents).
- Extrapyramidal symptoms (neurological SE) common so conventional antipsychotics are also known as neuroleptics.
- Block a variety of receptors: dopamine, acetylcholine, histamine, and norepinephrine
Current theory suggests that blockade of dopamine receptors suppresses symptoms of psychosis
Therapeutic Uses
- Schizophrenia
- Bipolar Disorder
- Tourette’s Syndrome
- Prevention of emesis: block dopamine receptors in the chemoreceptor trigger zone (CTZ) of the medulla
```
Examples of Conventional Antipsychotic Agents
-Chlorpromazine (Thorazine) ******for test
-Fluphenazine (Prolixin)
-Perphenazine (Trilafon)
-Thiothixene (Navane)
-Loxapine (Loxitane)
-Haloperidol (Haldol) *****for test
Pimozide (Orap)
```
52
Atypical antipsychotics~2nd generation
¥ Produce only moderate blockade of receptors for dopamine but has a much stronger blockade of receptors for serotonin
¥ Low risk of extrapyramidal symptoms
¥ Higher risk of diabetes, weight gain, dyslipidemia
¥ Now the first-choice antipsychotic agents
53
Extrapyramidal symptoms
Movement disorders resulting from effects of antipsychotic drugs on the extrapyramidal motor system
Exact cause unclear; blockade of dopamine receptors is strongly suspected
Four types of EPS occur: acute dystonia, parkinsonism, akathisia, and tardive dyskinesia
54
Acute Dystonia
- Develops within the first few days of therapy; often within hours of the first dose
- Severe spasm of the muscles of the tongue, face, neck, or back
- Oculogyric crisis: involuntary upward deviation of the eyes
- Opisthotonus: tetanic spasm of the back muscles causing the trunk to arch forward, while the head and lower limbs are thrust backward
- Laryngeal dystonia can impair respiration
- Requires rapid intervention
- Drug will be given to try treat EPS while you continue to take the drug (treat the symptoms)
- Initial treatment consists of anticholinergic medication, e.g. benztropine (Cogentin) or diphenhydramine (Benadryl) administered IM or IV; rapid symptom resolution
55
Parkinsonism
-Antipsychotic-induced parkinsonism is characterized by bradykinesia, mask-like faces, drooling, tremor, rigidity, shuffling gait, and stooped posture
¥ Parkinson’s Disease (PD) and neuroleptic-induced parkinsonism share the same symptoms
¥ Eating difficulty
¥ Anticholinergic drugs are used to control symptoms
¥ Resolves spontaneously
Akathisia
¥ Characterized by pacing and squirming brought on by an uncontrollable need to be in motion
¥ Usually develops within the first 2 months of treatment
¥ Beta blockers, benzodiazepines, and anticholinergic drugs are used to control symptoms
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Tardive Dyskinesia (TD)-
***this is the only EPS symptom where meds wont reverse these side effects and will talk about withdrawing the drug and prescribing something else
¥ Most troubling of the EPS
¥ Develops in 15% to 20% to patients during long-term therapy
¥ Risk is related to duration of treatment and dosage
¥ Often symptoms are irreversible
¥ Choreoathetoid (twisting, writhing, worm-like) movements of the tongue and face
¥ Lip-smacking and “fly-catching” movements
¥ Over time, TD produces involuntary movements of the limbs, toes, fingers, and trunk
¥ Eating difficulties → malnutrition, weight loss
¥ Cause complex, not completely understood
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Treatment of Tardive Dyskinesia
¥ No reliable treatment
¥ Prevention is key; frequent assessment for early signs of TD
¥ Withdraw antipsychotic agent if possible; use smallest dose for shortest time required
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Neuroleptic Malignant Syndrome
Adverse effect of conventional antipsychotic agents
-“Lead pipe” rigidity, sudden high fever, sweating, autonomic instability (dysrhythmias, fluctuations in blood pressure) confusion, seizures, and death
Treatment is supportive measures and immediate withdrawal of antipsychotic agent
-Benzodiazepines, fluid support, Dantrolene, bromocriptine, antipyretics- something for a fever
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Other Adverse Effects of Conventional Antipsychotic Agents
Anticholinergic effects: dry mouth, blurred vision, constipation, tachycardia, urinary hesitancy, photophobia d/t drug (that has anticholinergic effect) on and the anticholinergic that the pt is on.
Can cause.
-Alpha1-adrenergic blocking: orthostatic hypotension
- Histamine1 blocking: sedation- if given in one time does give at night time or break up in to small doses during the day.
- Neuroendocrine effects: gynecomastia, menstrual irregularities
- Seizures- lowers seizure threshold.
- Sexual dysfunction
- Agranulocytosis
- Severe dysrhythmias
- Severe sunburn with phenothiazines
Toxicity of Conventional
Antipsychotic Agents
-Large therapeutic index
-Lethal dose may be as high as 200 times the therapeutic dose
Drug interactions:
- Anticholinergic drugs
- CNS depressants- alcohol or antidepressants
- Levodopa and Direct Dopamine Receptor Agonists- for patients with parkinsons- increases the amount of dopamine
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Chlorpromazine (Thorazine) Low potency
Therapeutic uses: Schizophrenia, schizoaffective disorder, manic phase of bipolar disorder, suppression of emesis and intractable hiccups
◦ PO, PR, IM, IV
Adverse effects: (Most common)
sedation, orthostatic hypotension, and anticholinergic effects (dry mouth, blurred vision, urinary retention, photophobia, constipation, tachycardia)
◦ Lowers seizure threshold
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◦ Lowers seizure threshold
| } Haloperidol (Haldol) high potency
Therapeutic uses: Schizophrenia, acute psychosis, preferred drug for Tourettes Syndrome, intractable nausea/vomiting
◦ PO, IM, IV (not FDA approved)
Most common adverse effects: early extrapyramidal reactions (dystonia, parkinsonism, akathisia)
◦ Risk of TD same between high and low potency FGA’s
◦ Prolonged QT – get baseline and periodic ECG and K+ levels
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Atypical Antipsychotic Agents
| Second Gen
These agents have similar efficacy as typical agents in controlling positive symptoms
-Greater efficacy in controlling negative symptoms
- Fewer EPS and drugs are associated with a lower rate of relapse
- May cause weight gain, diabetes, dyslipidemia (can lead to CAD)
MOA:
- Block receptors for dopamine and serotonin
- Some blocking of norepinephrine, histamine, and acetylcholine
- Greater affinity for blocking of serotonin than dopamine, thus more acceptable side effect profile.
- Also approved to treat bipolar disorder.
Adverse Effects of Atypical Antipsychotic Agents:
¥ Seizures
¥ Diabetes: in extreme cases, DKA; manage with oral antidiabetic agents or insulin
¥ Weight gain: due to blocking of histamine receptors; may lead to Type II diabetes
¥ Dyslipidemia: monitor lipids
¥ Sedation & Orthostasis
¥ Dementia/Elderly increased risk of death
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Clozapine (Clozaril)
Second Gen-
¥ Treats schizophrenia
¥ May cause agranulocytosis in 1% to 2% of patients
¥ Agranulocytosis typically occurs during the first 6 months of treatment
¥ Risk of death is about 1 in 5000 due to septicemia
Etiology of agranulocytosis is unknown
¥ Monitor WBC, neutrophils
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Maintenance Therapy
¥ Schizophrenia is a chronic disorder that usually requires prolonged treatment
-Following control of an acute episode, antipsychotic therapy should continue for at least 12 months; withdrawal before this time is associated with relapse
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Depot Medications for Schizophrenia
Benefits of depot:
Prevent relapse, maintain highest level of functioning
-Lower risk of EPS
Examples of depot:
¥ Haloperidol deconoate (Haldol)
¥ Risperidone microspheres (Risperdal consta)
¥ Fluphenazine deconoate (generic only)
¥ Olanzapine pamoate (Zyprexa relprevv)
¥ Aripiprazole (Abilify maintena)
¥ Paliperidone palmitate (Invega Sustenna, Invega Trinza)
Long acting injectable formulations
- Drug levels remain stable
- Lower risk of adverse effects, including TD
- May help reduce relapse and improve adherence
- Given every 2-4 weeks IM
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Mgmt of Schizophrenia
```
¥ Drug Selection
◦ Atypical generally first choice
◦ Depends on situation
¥ Dosing
◦ Highly individualized
◦ Initially daily divided doses then once daily at bedtime
◦ Bedtime dosing may help promote sleep
◦ May be higher early in therapy
```
For long term therapy should use the lowest effective amount
Management of Schizophrenia
¥ Initial therapy
¥ Symptoms begin to resolve within 1-2 days
¥ Significant improvement is seen in 1-2 weeks
Maintenance therapy
¥ Reduce recurrence of acute episodes and maintain high level of functioning
Adjunctive therapy
Nursing Implications
- Patients need a thorough mental status exam and a physical exam.
- Determine VS, labs (CBC, lytes, evals of hepatic, renal and CV function).
- Watch for contraindications
- Promote adherence
- Minimize adverse effects and interactions
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Antidepressants
Psychotherapy AND pharmacotherapy Best results
- Monoamine hypothesis of depression
- A functional insufficiency of monoamine neurotransmitters (norepinephrine, serotonin or dopamine)
Treatment Modalities for Depression
- Pharmacotherapy
- Depression-specific psychotherapy
- Somatic Therapies
- Electroconvulsive therapy
- Transcranial magnetic stimulation
Relief of depression takes weeks to months; psychotherapy is a key element
***Important to assess for suicide risk****
Drug Selection/Managing Treatment
- Initial therapy
- 4-8 weeks to assess efficacy
- Start low gradually increase
If initial therapy is not effective
◦ Increase the dosage
◦ Switch to another drug in the same class
◦ Switch to another drug in a different class
◦ Add a second drug
Encourage patients to continue therapy even if symptom free
Suicide Risk with Antidepressants
- Antidepressants can increase the risk of suicide
- Higher risk among children, adolescents, and young adults <25
- Box Warning on all antidepressants
- Observe closely for suicidality, worsening mood, or changes in behavior
- Observe closely during initial therapy and with changes in drug or drug dosages
- Antidepressants can be used to commit suicide
- Prescribe the smallest number of doses
- Inpatient dosing should be directly observed to ensure ingestion (no “cheeking”)
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Antidepressants
Selective Serotonin Reuptake Inhibitors (SSRIs) ~First line treatment~
Serotonin Norepinephrine Reuptake Inhibitors (SNRIs)
Tricyclic Antidepressants (TCA)
Monoamine oxidase inhibitors (MAOI)
Atypical Antidepressants
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SSRI
Most commonly prescribed group of antidepressants
- Fluoxetine (Prozac, Sarafem) is prototype agent
- Fewer side effects than TCA & MAOI
Death by overdose extremely rare
Mechanism of Action:
- Blocks re-uptake of serotonin
- Does not block uptake of dopamine or NE
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Fluoxetine (Prozac)
Therapeutic Uses:
- Major depression
- Bipolar
- Obsessive compulsive disorder
- Panic disorder
- Bulimia
- PMDD
Pharmacokinetics:
- Well absorbed orally even with food
- Prolonged half life
- 4 weeks to produce steady state effects
Adverse Effects:-most common
- Sexual dysfunction
- Nausea
- Headache
- CNS Stimulation (nervousness, anxiety, insomnia)
- Weight gain
- Increased bleeding risk
- Serotonin syndrome
- Withdrawal syndrome
- Dizziness, HA, nausea, sensory disturbances, tremor, anxiety and dysphoria
Taper the dose slowly
- Selective Serotonin Reuptake Inhibitors (SSRI) Drug :Interactions
- MAOIs
- Tricyclic antidepressants
- Antiplatelets and anticoagulants
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Tricyclic Antidepressants (TCA)
Amitriptyline (Elavil): prototype agent
Tricyclic anti-depressants (TCAs) – named for three ring chemical structure
Mechanism of action:
Block neuronal reuptake of two monoamine transmitters – norepinephrine and serotonin
-Also blocks receptors for histamine and acetylcholine
-Although fewer SE and less dangerous than MAO inhibitors there still are significant SE.
Therapeutic Uses
- Depression
- Bipolar disorder
- Fibromyalgia
- Neuropathic pain
- Insomnia
- ADHD
- OCD
- Migraine HA prophylaxis
Adverse Effects
- Anticholinergic effects
- Block muscarinic cholinergic receptors
- Dry mouth, blurred vision, photophobia, constipation, urinary hesitancy and tachycardia
- Orthostatic hypotension
- Block alpha1-adrenergic receptors on blood vessels
- Cardiac toxicity
- Seizures
- Sedation
- Hypomania
- Suicide risk
```
Drug Interactions:
¥ Monoamine Oxidase Inhibitors
-Severe hypertension
-Anticholinergic agents
-CNS depressants
-Toxicity/Overdose
```
Overdose
Overdose is life threatening
-Related to anticholinergic blockade and cardiotoxicity
-Treatment is gastric lavage and activated charcoal
-Treat dysrhythmias
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Monoamine Oxidase (MAO) Inhibitors
2nd or 3rd choice antidepressants
-High risk of triggering hypertensive crisis
Used for atypical depression
MAO – an enzyme found in the liver; converts monoamine neurotransmitters (NE, serotonin, and dopamine) into inactive products
By inhibiting MAO, drug increases NE and serotonin, intensifies transmission at receptor
- Inhibition is irreversible
- Must wait for synthesis of new MAO molecules, may take two weeks
Therapeutic Uses
Reserved for patients who have not responded to TCAs, SSRIs and other safer drugs
-Atypical depression
Adverse Effects
- CNS stimulation
- Orthostatic hypotension
- Hypertensive Crisis from dietary Tyramine
- Rigid dietary restrictions (Tyramine) – all cheeses, figs, bananas, caffeine, liver, chianti
Multiple Drug Interactions
- Indirect-acting Sympathomimetic Drugs
- TCAs
- SSRIs
- Antihypertensive drugs
- Meperidine
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Bupropion (Wellbutrin)
Atypical Anti-depressant
- Similar in structure to amphetamines
- Effects begin in 1-3 weeks
- Mechanism unclear
- Does not decrease sexual interest; may increase sexual desire
- Zyban formulation: used to help quit smoking
Adverse Effects:
-Seizures – when dosage is too high
Common: agitation, H/A, dry mouth, constipation, weight loss
Drug Interactions
- MAO’s increase risk of Bupropion (Wellbutrin) toxicity – discontinue two weeks before starting bupropion
Nursing Implications
-BEFORE administration
-Obtain complete list of medications
-Obtain baseline vital signs, heart rhythm
-Assess mental status and thoughts of suicide
TCAs: smoking = decreased effectiveness
AFTER administration
- Vital signs, heart rhythm
- Check mental status & suicidal thoughts
- Orthostatic hypotension precautions
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Patient education and Antidepressants
¥ Take exactly as prescribed
¥ Symptoms will persist up to 8 weeks
¥ Keep follow-up appointments
¥ Take medication even if feeling well
Missed dose: take as soon as possible unless it is almost time for next dose then just take next dose do not double up
May need to be gradually discontinued
- Avoid driving, operating machinery until adjusted to medication and side effects known
- Avoid alcohol (increases drowsiness)
- If patient is transitioning off antidepressant to an MAOI to wait 14 days to start new drug
- Can cause serotonin syndrome
- Wear a medical alert bracelet
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Drugs for Bipolar
what is Bipolar: Severe biologic illness-Recurrent fluctuations in moods; Alternate between elevated mood and depressed
Treatments:
Mood stabilizers
¥ Relieve symptoms during manic and depressive episodes
¥ Prevent recurrence
¥ Do not worsen symptoms or accelerate cycling
Antipsychotics
¥ Control symptoms during severe manic episodes
¥ Used in combination with a mood stabilizer
Antidepressants
¥ Combined with a mood stabilizer to prevent mania or hypomania
Benzodiazepines- during manic acute episodes
¥ Used for sedation
Drug Selection
- Acute Therapy: Manic episodes
- Lithium (drug of choice) or Valproate
- Second-generation antipsychotic (atypical)
- +/- benzodiazepine
Depressive episodes Antipsychotics
- Mood stabilizer
- Second-generation antipsychotic
- +/- antidepressant
Long-term Preventative Therapy
- Purpose prevent recurrence
- Mood stabilizers—choice based on what worked during acute phase
- Adherence is key
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Mood Stablizers
Lithium, Valproic acid, Carbamazepine
Lithium- works the best, first drug of choice
Low therapeutic index
Therapeutic Uses
- BPD
- Drug of choice for controlling acute manic episode and long term prophylaxis against recurrence
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Lithium
Mechanism of action unknown
Pharmacokinetics
- PO
- Well absorbed evenly distributed
- Short half life – requires divided daily doses
- Excreted in kidneys -caution in renal impairment
- Renal excretion of lithium is affected by blood levels of sodium
- ↓sodium level → ↓lithium excretion
The kidneys process lithium and sodium the same way so when sodium is low it will hold on to lithium
- When the kidneys sense sodium levels are inadequate, they retain lithium in an attempt to compensate
- Dehydration lithium toxicity
- Plasma lithium levels
- Maintenance levels 0.4-1.0 mEq/L
Draw levels in the am 12 hours after the evening dose trough 30 minutes before next dose
- Measure every 2-3 days at beginning of treatment
- During maintenance draw levels every 3-6 months
- Lithium levels above 1.5 mEq/L can cause significant toxicity
Effects with therapeutic Lithium levels:
- Gastrointestinal effects- N/V, bloating
- Fine hand tremors- can inhibit signs of daily living- give low dose of beta blocker and see if it balances out
- Polyuria- inhibits ADH
- Thirst
- Renal toxicity
- Goiter and hypothyroidism
- Teratogenesis- increases lithium in the breast feeding child
Effects with excessive Lithium Levels
- Persistent GI upset
- Confusion
- Hyperirritability of muscles
- ECG changes
- Sedation
- Blurred vision
- Seizures
- High output of dilute urine
- Ultimately death
Drug interactions
- Diuretics
- Nonsteroidal anti-inflammatory drugs (NSAIDs) increase lithium levels by 60%
- Anticholinergic drugs
Preparations, dosage, and administration
- Lithium carbonate (tablets)
- Lithium citrate (syrup)
Dosage is highly individualized
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Valproic Acid (Depakote)- anticonvulsant
```
Drug of choice for many patients
¥ Anti-seizure medication
¥ Increases level of GABA
¥ Control symptoms in acute manic episodes and prophylaxis against recurrent episodes of mania and depression
¥ Works faster
¥ Higher therapeutic index than lithium
¥ Adverse effects
¥ Thrombocytopenia
¥ Pancreatitis
¥ Liver failure
¥ Teratogenic
¥ GI – use enteric coated formulation
¥ Weight gain
```
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Antianxiety Medications
Most commonly used drug classes:
- Benzodiazepines – used for general anxiety disorder & panic disorder
- SSRIs effective in all anxiety disorders
Psychotherapy along with drug therapy is a key component of successful management
-Unrealistic or excessive anxiety about >1 event or activity lasting 6 months or more
Treatment
¥ 1st line: SSRI, SNRI, buspirone
¥ 2nd line: benzodiazepines
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Generalized Anxiety Disorder
| -Antidepressants
```
For long-term management, not acute episodes
¥ Can take several weeks to take effect
¥ SNRI’s and SSRI’s
¥ Venlafaxine (Effexor ER)
¥ Duloxetine (Cymbalta)
¥ Paroxetine (Paxil)
¥ Escitalopram (Lexapro)
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Buspirone (BuSpar)
Anxiolytic, not structurally related to benzos
- Not a CNS depressant
- Similar anxiolytic efficacy compared to benzos---some question about the evidence
Effects develop slowly
- Not for prn dosing
- Start therapy 2-4 weeks prior to initiating benzodiazepine taper
- No abuse potential
- Well absorbed
Administration with food delays absorption but enhances bioavailability
Adverse Effects
- Nervousness and excitement
- Dizziness
- Nausea
- Headache
Drug and Food Interactions
- Erythromycin- enhance concentration
- Ketoconazole- enhance concentration
- Grapefruit juice- enhance concentration
Has been used for up to one year without evidence of tolerance
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Panic Disorder treatments
¥ Peak intensity within 10 minutes, can last up to 30 minutes
¥ Patients often think symptoms to be a heart attack
¥ Agoraphobia occurs in 50% of the patients with Panic Disorder
Treatment
-Cognitive behavioral therapy, exercise, avoid sympathomimetics & caffeine
- Antidepressants: SSRIs, SNRIs, TCAs and MAOIs
- Benzodiazepines: alprazolam (Xanax), clonazepam (Klonopin), lorazepam (Ativan)
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Obsessive-Compulsive Disorder (OCD)
Obsession: Recurrent persistent thought impulse or mental image
Compulsion:Ritualized behavior in response to the obsession
Treatment
Behavioral therapy: important
- SSRIs
- TCA: clomipramine
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Social Anxiety Disorder (SAD)
Intense irrational fear of situations in which one may be scrutinized by others
Treatment ~ individualize
- Nondrug Therapy/Psychotherapy
- SSRIs
- Benzodiazepines
- Propanolol (Inderal): non-selective beta adrenergic antagonist
- Performance anxiety
- Small dosage taken 1-2 hours before performance
WHY BETA BLOCKER?
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Post-traumatic Stress Disorder (PTSD)
Develops following a traumatic event
- Fear, helplessness or horror
- Re-experiencing the event
- Avoidance of reminders
- Persistent state of hyperarrousal
Treatment
- Psychotherapy
- Drug Therapy
- SSRI’s
