PHARMACOLOGY STUDY GUIDE: WEEK 4
(CHAPTER 37 - DRUGS FOR VIRAL INFECTIONS)
(CHAPTER 38 - DRUGS FOR VIRAL NEOPLASIA)
(CHAPTER 39 - DRUGS FOR ALLERGIC RHINITIS & THE COMMON COLD)
(CHAPTER 40 - DRUGS FOR ASTHMA & OTHER PULMONARY DISORDERS)
(CHAPTER 12 - CHOLINERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM)
(CHAPTER 13 - ADRENERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM)
CHAPTER 37 - DRUGS FOR VIRAL INFECTIONS
VIRAL INFECTIONS: - A proliferation of a harmful virus inside your body. Viruses cannot reproduce without the assistance of a host.
TACHYPNEA: abnormally rapid breathing, about RATE
DYSPNEA: difficult or labored breathing, about EFFORT
early dyspnea: - having trouble completing sentences, trying to talk and catching your breath in between
⤷ assess activity, O2, myelosuppression
⤷ monitor hemoglobin & hematocrit [h&h]
CHALLENGES OF ANTIVIRAL THERAPY
• viruses mutate rapidly, and drug become ineffective
• difficult for drug to find virus without injuring normal cells
• each antiviral drug specific to one virus
TREATMENT FAILURES
• Common with antiretroviral therapy: - patient nontolerance of AE
- patient nonadherence to complex regimen
- emergence of resistant strains
- genetic variability
• Therapy always changing
• Stay current with latest treatments
AUDIO - CH 37: DRUGS FOR VIRAL INFECTIONS
• VIRAL INFECTION: HIV drugs
• GOAL OF HIV DRUGS: reduce viral load of HIV virus
• How do we know if the medication is working? - Because the T4 lymphocyte count going ↑ or staying the same & viral load ↓
• How do we know that drug is not working? (resistance) - because of the viral load, HIV count is going ↑ & lymphocyte count (T cell) ↓
• HIV is contracted by transmission blood or body fluid (semen, breast feeding) - you cannot get it by sweat or by kissing unless someone has bad gingivitis.
• Immune system disintegrates because of HIV - gradual destruction of immune system
• HIV: 2 RNA strands with some replication enzymes inside a capsid (container)
[This capsid looks for T lymphocytes that has CD4 receptor sites]
• CD4 receptor site: target host cell for HIV virus
• When HIV capsid finds the CD4 receptor site on T cell, latches onto that and penetrate into T cell.
• Once the capsid penetrated to the host hell (T cell) then capsid uncoats (dissolve), there is 2 RNA strands and replication enzymes:
- reverse transcriptase
- integrase
- protease
• Once the RNA HIV has been released from capsid, first thing that happens is that the reverse transcriptase changes the single strand of RNA and creates double
strand of DNA.
• Once double strand DNA was created, the enzyme integrate takes the double strand of HIV DNA and integrates it into the DNA of T cell, splice it and attach it.
Once replicated, now it’s up to protease to take the DNA and make it single strand and create new single strand RNA genomes.
VIRAL LOAD: measurement of how much HIV is in the system
♡ Highly Active Antiretroviral Therapy (H A A R T): aggressive treatment with multiple drug to treat HIV (given simultaneously)
GOAL OF HAART: to reduce the plasma HIV RNA to its lowest possible level
DISADVANTAGE/ DRAWBACK OF HAART: affects kidney and liver (toxicity)
▪ LIVER: HEPATOTOXICITY SE: - ↑ liver enzyme (liver function enzyme)
AE: > jaundice
> ↑ ammonia levels causing CNS problems
> delusion, coma, bleeding times
▪ KIDNEY: NEPHROTOXICITY SE: - creatinine trending ↑
AE: > ↑ creatinine, ↑BP (HTN)
> ↓ UO = ↑K+ (hyperkalemia)
> acidosis
MOST COMMON SE: • nausea d/t medications taken on empty stomach
• rash SE: hypersensitivity AE: anaphylaxis
• bone marrow suppression: (h&h - anemia = fatigue/weakness)
• prone to infection: fungal infection (candidiasis - white patchy growth on tongue, specific fungal
infection under skin folds or perineum with distinctive smell)
• thrombocytopenia (↓platelets = ↑ bleeding)
• headache usually occurs with AZT SE: headache. AE: lactic acidosis (causes generalized ↓BP [hypotension]) = causes arterial
vasodilation which causes blood flow to go up into the brain that ↑ ICP which causes headache
• CNS effects: neurotoxicity - numbness, tingling of hands and feet, insomnia, nightmare
1.
VIRUS
A. Mature Particles: virion
B. Can cause serious disease & require aggressive therapy
⤷ ex. HIV: fatal if left untreated
HERPES: significant pain & disability if left untreated
C. Mutate rapidly ⤍ drug becomes less effective
D. Difficult for drugs to find virus without injuring normal cells
E. Each antiviral drug ⤍ specific to 1 virus
2.
HIV
A.
B.
C.
D.
E.
F.
G.
target CD4 receptors on T4 lymphocytes
1. use reverse transcriptase - make viral DNA from RNA
Virions bud from host cell
1. enzyme protease enables virion to infect other T4 lymphocytes
2. RESULT: gradual destruction of immune system
called “RETROVIRUS” because of reverse synthesis process
NO cure yet
1. some therapeutic success • people live symptom-free longer
• rate of transmission from mother ⤍ newborn { reduced
• 70% decline in death rate in the U.S
⤷ incidence of infections still very high in African nations
Phases of HIV Therapy
1. LATENT PHASE ⤍ virus lies dormant
- people often unaware they have HIV
2. Once diagnosis confirmed, decision made about starting or delaying treatment
3. Current protocols: • defer treatment in asymptomatic adults who have CD4 counts > 350 cells/mcL
• therapy is initiated when CD4 is < 200 cells/mcL or symptoms appear
Therapeutic Goal: 1. Reduce HIV RNA load in blood
⤷ undetectable level: < 50 copies/mL
2. ↓ risk of transmission from mother ⤍ child
3. ↑ quality of life
4. ↑ life span
- ↓ HIV RNA load in load in blood, ↓ risk of transmission from mother ⤍ child
- ↑ quality of life, ↑ life span
Pharmacotherapy may be initiated: 1. acute phase (symptomatic)
2. chronic phase (asymptomatic)
3. Highly Active Antiretroviral Therapy (HAART)
A. 5 Drug classes used in various combinations: 1. Nucleotide Reverse Transcriptase Inhibitor (NRTIs)
2. Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI)
3. Protease Inhibitor
4. Entry Inhibitors – includes fusion inhibitors & CCR5 antagonist
5. Integrase Inhibitors & other miscellaneous antivirals
B.
Common with antiviral therapy: 1. pt. nontolerance of adverse effects
2. pt. nonadherence to complex regimen
3. emergence of resistant strains
4. genetic variability ⤍ people react differently to drugs based on genetic makeup
- Therapy is always changing
- stay current with latest treatment
4. HIV-AIDS Antiretroviral Classifications
MOA: A. Nucleotide Reverse Transcriptase Inhibitor (NRTIs)
⤷ resemble natural building blocks of DNA
B. Nonnucleoside Reverse Transcriptase Inhibitor (NNRTIs)
⤷ target the enzyme needed for reverse transcriptase
C. Protease Inhibitors
⤷ block the viral enzyme protease, inhibiting final assembly of HIV virions
D. Entry Inhibitors
⤷ block the entry of viral nucleic acid into the T4 lymphocyte
E. Integrase Inhibitor/ Miscellaneous Antivirals
⤷ Integrase enzyme insert its viral DNA strand into human chromosome ⤍ Integrase Inhibitors …INHIBIT/ stop that from happening
I.
NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS [NNRTIs]
1. Prototype: efavirenz (Sustiva) - #1 drug in initially treating HIV
2. rilpivirine (Edurant)
PHARMACOLOGIC CLASS: NNRTI - resistance to NNRTI can develop rapidly
THERAPEUTIC CLASS: Antiretroviral
- HOW TO KNOW IF RESISTANCE DEVELOPED?: • CD4 counts going ↓,
• Viral load going ↑ = ✘ drug Is not working
INDICATION: • in combination with other antivirals in treatment using HAART (Highly Active Antiretroviral Therapy)
• HIV
• ADVANTAGE: once-daily dosing & penetration into cerebrospinal fluid
• preferred drug for the initial therapy of HIV Infection
MOA: - bind directly to reverse transcriptase, disrupting enzyme’s active site
- inhibiting reverse transcriptase
CONTRAINDICATION: ▪ efavirenz is a known teratogen in laboratory animals
⤷ causing neural tube defects
▪ must not be given to pt. who may become pregnant
PREGNANCY CATEGORY: X - in first trimester
SE: rash (must be monitored carefully to prevent development of severe blistering) AE: > Steven-Johnson Syndrome
> CNS adverse effects are observed in at least 50% of pt when
first initiating therapy ⤷ take at night or AM depending on CNS S/S
⤷ sleeping disorders/nightmares/ dizziness/ ↓ concentration
⤷ symptoms diminish after 3-4 weeks of therapy
ADMINISTRATION ALERTS: ▪ EMPTY STOMACH
▪ administer at BEDTIME to limit adverse CNS effects
⤷ can be given in daytime too…just monitor the SE & AE
DRUG-DRUG: • St. John’s Wort ⤍ ↓antiretroviral activity
• pts. taking antiepileptic medications metabolized by the liver need to have drug levels monitored because it can ↑ incidents of seizures
• avoid alcohol
II.
NUCLEOSIDE & NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTI)
1. Prototype: zidovudine (AZT, Retrovir) - first drug invented to fight HIV, strains of HIV developed resistance to AZT
- first choice therapy for the prophylaxis of mother to child HIV transmission
2. tenofovir (TDF, Viread)
PHARMACOLOGIC CLASS: NRTI
THERAPEUTIC CLASS: Antiretroviral
INDICATION: - used with other antiretrovirals for symptomatic & asymptomatic HIV-infected pt.
- postexposure prophylaxis in HIV-exposed healthcare workers
- reduce transmission rate from HIV + mother ⤍ fetus
MOA: virus mistakenly uses zidovudine as nucleoside, thus creating defective DNA strand
SE: • anorexia, nausea, diarrhea
AE: - anemia
}
• fatigue, generalized weakness
}
• opportunistic infection
> neutropenia
} - bone marrow suppression [ severe anemia, neutropenia]
• unusual bruising, bleeding gums
> thrombocytopenia }
• HEADACHE usually occurs with zidovudine (AZT, Retrovir)
> lactic acidosis [HA, ↓BP, asymptomatic hypotension]
BLACK BOX WARNING: ▪ rare cases of fatal lactic acidosis with hepatomegaly & steatosis (fat build up in liver)
▪ Bone Marrow Suppression may result in neutropenia, severe anemia, thrombocytopenia
CONTRAINDICATION: • because the drug can suppress bone marrow fracture
⤷ used in caution in pt. with preexisting anemia, neutropenia, thrombocytopenia
• blood counts & other lab blood tests should be monitored frequently during therapy to prevent hematologic toxicity
• pt. with significant renal or hepatic impairment require a reduction in dosage, can accumulate to toxic levels
• hx. of kidney/ liver failure
NURSING RESPONSIBILITIES: - monitor h&h, monitor leukocytes
ADMINISTRATION ALERTS: - EMPTY STOMOACH WITH FULL FLASS OF WATER
- AVOID ADMINISTERING WITH FRUIT JUICE
▪ because zidovudine was used at beginning of AIDS endemic, resistant HIV strains have become common
⤷ zidovudine (AZT, Retrovir) is NO LONGER 1st drug of choice due to potential for resistance
DRUG-DRUG: • St. John’s Wort ⤍ ↓antiretroviral activity [all HAART therapy are affected by St. John’s Wort – for depression]
MYOPATHY: affects production of coenzyme Q10 - responsible for providing energy with skeletal muscles
III.
PROTEASE INHIBITORS (PIs)
1. Prototype: lopinavir/ ritonavir (Kaletra) - combination of TWO generic drugs
PHARMACOLOGIC CLASS: Protease Inhibitor
THERAPEUTIC CLASS: Antiretroviral
INDICATION: • used in combination with other antiretrovirals for HIV pts.
• HIV
MOA: inhibits HIV protease
SE: - MOST COMMON PROBLEM IS DIARRHEA
AE:
▫ diarrhea then it also has something to do with bone marrow suppression
> diarrhea ➜ dehydration that causes ↓BP
> diarrhea ➜↓ K+ that causes cardiac dysrhythmias
> diarrhea ➜ loss of bicarb that causes metabolic acidosis
▫ n/v/d dyspepsia, general fatigue
> hyperglycemia
CONTRAINDICATION: pt. with diabetes should be monitored regularly because of diabetes
NURSING RESPONSIBILITIES: ▪ monitor CD4 counts: - If CD4 counts is going ↓, viral load going ↑ = DRUG IS NOT WORKING
- If CD4 counts is going ↑ and viral load going ↓ = DRUG IS WORKING
▪ monitor CBC: need to see if bone marrow suppression is in place
▪ monitor liver function test: hepatotoxicity
▪ renal function (creatinine): nephrotoxicity
⧫
⧫
⧫
⧫
⧫
nausea (can lead to anorexia) ⇨ PO intake (taking on empty stomach ⇨ anorexia (losing appetite due to nausea)
monitor VS ⇨ diarrhea ⇨ (dehydrated) ↓BP ⇨ ↑HR
can develop secondary infection which can lead to fever (viral infection don’t cause temperature but bacterial infections do)
RASH: rashes with small blisters = signs of Steven Johnson Syndrome
monitor blood abnormalities: - low grade fever (neutropenia)
- fatigue (anemia)
- bleeding/bruising (thrombocytopenia)
DRUG-DRUG: • St. John’s Wort
♡ RN APPLICATION - NURSING DX.
a. fatigue ⤍ activity intolerance ⤍ impaired skin integrity (pressure ulcers) ⤍ immobility
b. anxiety ⤍ ↑HR
⤷ fatigue
c. Imbalanced Nutrition ⤍ nausea/vomiting ⤍ less than body requirements
d. Deficient Fluid Volume ⤍ nausea/vomiting ⤍ dehydration
e. Diarrhea ⤍ ↓ BP
f. Impaired Oral Mucous Membrane
g. stigma of HIV ⤍ social isolation
h. confusion (acute or chronic) ⤍ A&O x 4 (assess for confusion)
♡ NURSING RESPONSIBILITY
a. monitor VS ⤍ esp. FEVER (101F) ⤍ opportunistic infection
[because bone marrow suppression = ↓WBC]
b. report fever, dyspnea (SOB), ↑HR, dizziness (syncope), change in behavior
c. monitor labs: • LFTs ⤍ hepatoxicity (avoid alcohol)
• creatinine levels ⤍ renal impairment
• CBC ⤍ opportunistic infection
• CD4
• HIV viral load
• glucose ⤍ hyperglycemia (diabetes)
♡ PATIENT TEACHING
a. report fever
b. dizziness/syncope
c. inability to maintain hydration/nutrition (because of N/V)
d. yellow sclera ⤍ liver impairment
e. abdominal pain
f. light/gray/clay colored stool ⤍ hepatitis
g. numbness of extremities (feet/hands)
h. no alcohol, no acidic beverage
i. take with food or milk (if nausea)
⤷ dependent on tolerance because ideally take on empty stomach & H20
♡ HERPES VIRUS INFECTION
a. Family of DNA viruses….
- can cause repeated blister like lesions on the skin, genitals & other mucosal surfaces
Antiviral drugs lower frequency of acute episodes & diminish intensity of acute disease
- Relieve acute symptoms, prevents reoccurrences
- Does NOT provide cure
b.
IV.
NUCLEOSIDE ANALOG
1. Prototype: acyclovir (Zovirax) - Zovirax has a short half-life ROUTE: PO/IV
2. Valacyclovir (Valtrex)
PHARMACOLOGIC CLASS: Nucleoside Analog
THERAPEUTIC CLASS: Antiviral for herpesviruses
INDICATION: • herpes virus - DRUG OF CHOICE
• most effective against HSV-1 & HSV-2
• only effective with high doses against CMV & Varicella Zoster/ chicken pox
MOA: preventing viral DNA synthesis
⤷ ↓ duration & severity of acute herpes episodes
SE: ▪ ↓UO ⤍ ↑creatinine
AE: > nephrotoxicity (SE: ↓UO, HTN, AE: ↑creatinine)
▪
paresthesia (numbness/tingling)
> neurotoxicity (hearing problems, numbness in hands and feet) are possible when the medication is given IV
NURSING RESPONSIBILITY: • check values for kidney function test (↑ BUN & ↑ Creatinine)
• neurochecks
ADMINISTRATION ALERT: - when given IV, drug may cause painful inflammation of vessels at site of infusion
- administer around the clock, even if sleep is interrupted (wake them up to administer) because if its not administered on regular
basis, the virus can develop quickly and become resistant to Zovirax
- WITH FOOD
DRUG-DRUG: • concurrent use of acyclovir (Zovirax) with nephrotoxic agents should be avoided
⤷ ex. aminoglycoside (Gentamycin) - monitor peak/troughs
V.
DRUGS FOR INFLUENZA
1. amantadine (Symmetrel) ROUTE: PO
2. rimantadine (Flumadine) ROUTE: PO
3. oseltamivir (Tamiflu)
PHARMACOLOGIC CLASS: Drugs for Influenza
• Best approach ⤍ vaccination for prevention
• Antivirals to prevent/ ↓ severity pf acute symptoms
VI.
DRUGS FOR VIRAL HEPATITIS
1. Hepatitis A immunoglobulins (HA Ig)
2. Hepatitis B immunoglobulins (HB Ig)
3. Hepatitis C - Interferon
PHARMACOLOGIC CLASS: Viral Hepatitis
▪ A, B, C types are primary
▪ causes inflammation, necrosis of liver cells
▪ Vaccinations available for A & B NOT C
▪ prophylaxis or postexposure treatment: - Hepatitis A immunoglobulin (HA Ig)
- Hepatitis B immunoglobulin (HB Ig)
▪ Symptomatic treatment for chronic hepatitis
▪ Hepatitis C - Interferon
CHAPTER 38 - DRUGS FOR VIRAL NEOPLASIA
VIRAL NEOPLASIA
⤷ new cells that are growing fast that are abnormal
CANCER based on cells that replicate – replicated abnormally
CANCER (Carcinoma) characterized by rapid, uncontrolled cell division: cells lose normal functions and invade normal tissues
METASTASIS: cancer cells travel to another location
TUMOR (Neoplasm/ a mass/ a swelling): • Named for tissue where it originates
- suffix – oma, as in lymphoma
• May be solid masses or disseminated in blood
CHEMOTHERAPY: either to stop the replication of cells or to slow it down
CHEMOTHERAPY HAS 3 GENERAL GOALS: ▪ to CURE (1ST GOAL)
▪ to CONTROL - (2ND GOAL) slow it down/ preventing the growth
▪ for PALLIATION: shrinks size of tumor/ relieves pain – improving quality of life
CANCER – chronic disease process – something that people have for years until they die
▫ LATE STAGES = give chemotherapy as palliation (shrinks size of tumor, relieves pain) = just to give loved one little more time
▫ ALKYLATING AGENTS: - work independently in the cell cycle – ex. Cyclophosphamide (Cytoxan) (neoplastic drugs/immunosuppressants/ immunomodulators)
doesn’t matter where cell cycle is, it works in general)
- form bonds with DNA, prevent cell division
GROWTH FRACTION: measure of the number of cells under going mitosis in the tissue. It is the ratio of the number of replicating cells to the number of resting cells.
- Antineoplastic drugs are more toxic to tissues and tumors with high growth fractions.
• CELLS WITH HIGH GROWTH FRACTION: leukemias and lymphomas (hair loss/ alopecia)
• CELLS WITH LOW GROWTH FRACTION: solid tumor = breast and lung cancer
▫ ANTINEOPLASTIC: target cancer cells and some target normal cells as well, medications used to treat cancer, medication that stops the growth of the cells
ALL ANTINEOPLASTIC DRUGS: - cause hepatotoxicity and nephrotoxicity
- MYELOSUPPRESSION (condition in which bone marrow activity is ↓, resulting in fewer RBC, WBC, and platelets)
▫ ONCOLOGY/ NEOPLASTIC DRUGS: similar SE & AE
MOST COMMON AE: • nausea (emetogenic potential/ emetic: high risk of causing n&v)
• alopecia
• mucositis
• give antiemetics, contact dietary – optimize calories able to consume – encourage ↑ caloric drinks with ice (cooling effect)
• bone marrow suppression (myelosuppression) (↓ RBC, WBC, platelets)
CONTRAINDICATION: myelosuppression
▫ VESICANTS: - agents that cause serious tissue injury if they escape (extravasates) from an artery or vein during infusion or injection
- Drugs that can result in tissue necrosis or formation of blisters when accidentally infused into tissue surrounding a vein
▫ EXTRAVASATION vs INFILTRATION: - the difference between an infiltration and extravasation is the type of medicine or fluid that is leaked
- EXTRAVASATION: actual medication is leaking, leakage of IV fluid infused
- INFILTRATION: fluid is leaking (NS, LR)
- Both are caused when the vein leaks or the IV catheter comes out of the vein; however, extravasation is far more severe
- Make sure before giving IV push, check for patency (you can push 5-10cc in without any problem)
- REMEMBER: it can affect hormones related to reproduction. Antineoplastics can result to infertility
CANCER (Carcinoma)
A. characterized by rapid, uncontrolled cell division
B. cell lose normal function & invade normal tissues
C. METASTASIS: cancer cell travel to another location
D. Multiple Drug Strategy: • affect different stages in neoplastic cell cycle
• using different MOA ⤍ ↑cell kill
• combinations allow for lower doses
⤷ reduce toxicity
E. Serious Toxicity Limits Therapy - difficult to kill cancer cells without killing normal cells
F. ADVERSE EFFECTS of therapy: 1. ALOPECIA
2. Mucositis (painful ulcerations, GI bleeding, diarrhea)
3. N/V
- drugs that are effective against N/V
⤷ drugs with high emetic potential pretreated with antiemetics - (Zofran, Compazine, Reglan, Ativan)
4. Bone Marrow Depression
a. anemia
⤍
b. leukopenia
⤍
c. thrombocytopenia ⤍ treated with bone marrow transplantation, platelet infusions or growth factors
5. If neutropenia occurs ➜ wait 24hrs. to administer filgrastim (Neupogen) - ↑ neutrophil
⤷ < 1,500 cells/mL - infection risk ↑
G. Vesicants (blistering agents)
⤷ can cause tissue injury if extravasation occurs
- know emergency treatment before giving vesicant IV
H. Long term consequences
• possible infertility
• ↑ risk for secondary tumors
1.
VII.
ANTINEOPLASTICS
MOA: A. ALKYLATING AGENTS - prevent cell division by interfering with DNA
B. ANTIMETABOLITES - disrupt metabolism of nucleic acid
C. ANTITUMOR ANTIBIOTICS - antibiotics that kill some cancer cells
D. NATURAL PRODUCTS - from plants ⤍ prevent division of cancer cell
E. HORMONES & HORMONE AGENTS - slow growth of hormone-dependent tumors
F. BIOLOGIC RESPONSE MODIFIERS & MONOCLONAL ANTIBIOTICS – enhance body’s ability to remove cancer cells
DRUG-DRUG: - ANTINEOPLASTICS & NSAID = MYELOSUPPRESSION
ALKYLATING AGENTS
1. Prototype: cyclophosphamide (Cytoxan) - nitrogen mustard
2. cisplatin (Platinol)
PHARMACOLOGIC CLASS: Alkylating Agents
THERAPEUTIC CLASS: Antineoplastic
ALKYLATING AGENTS: - broad spectrum of activity
- act by changing structure of DNA in cancer cells
- can cause significant bone marrow suppression
INDICATION: • treats wide variety of cancer: ▪ Hodgkin’s disease
▪ lymphoma
▪ Ovarian cancer
▪ breast cancer
▪ multiple myeloma
MOA: attaches to DNA & disrupts replication
SE: • n/v/d
AE: nausea > bone marrow suppression
• alopecia, anorexia
• gastrointestinal mucositis
• ↓ WBC, RBC, platelets
> myelosuppression
> alopecia
PREGNANCY CATEGORY: D
CONTRAINDICATION: - those who have active infections
- severely suppressed bone marrow/ myelosuppression
ADMINISTRATION ALERT: - monitor platelet counts prior to IM administration
⤷ (IM puncture tissue which leads to bleeding, if platelet count is ↓, it will ↑ bleeding)
NURSING RESPONSIBILITY: 1. Hold & notify md if ↓ RBC, WBC, platelets
2. use caution with hepatic or renal impairment, recent steroid therapy, leukopenia, or thrombocytopenia
3. Hydrate pts. with IV or oral fluids before starting chemotherapy
4. Advise pt. to avoid crowds & those with respiratory infections
5. Monitor nutritional intake
6. Assess for N/V
⤷ be prepared to administer antiemetic drugs (Zofran, Compazine, Reglan, Ativan)
7. Offer ice chips or ice pops ⤍ relieve mouth pain
8. Assess skin injury
9. Monitor signs of hearing loss
10. Inform pt. potential adverse impact on fertility
11. Maintain strict medical asepsis
VIII.
ANTIMETABOLITES
1. Prototype: methotrexate (Trexall) - folic acid analog - drug for organ rejection
2. Fluorocil (5-FU, Adrucil) - pyrimidine analog
PHARMACOLOGIC CLASS: Antimetabolite
THERAPEUTIC CLASS: Antineoplastic
INDICATION: • treats bone cancer • breast carcinomas
• leukemias
• lung carcinomas
• head & neck cancers
• lupus, rheumatoid arthritis
MOA: - blocks synthesis of folic acid (Vitamin B9) to inhibit DNA replication
- disrupts metabolic process of cancer cells
SE: • leukopenia (neutropenia), anemia, thrombocytopenia
AE: bone marrow suppression
• blisters in mouth (mucositis)
GI ulceration ⤍ bleeding
• n/v/d
• anorexia, alopecia
• rash with blisters > Steven Johnson Syndrome
• ↓ CBC
PREGNANCY CATEGORY: X
CONTRAINDICATION: - pregnancy/ myelosuppression
- leukopenia (neutropenia), anemia, thrombocytopenia
NURSING RESPONSIBILITY: 1. monitor photosensitivity
2. teach pt. to use good oral hygiene & encourage mouth rinses
3. monitor IV sites frequently for extravasation
ADMINISTRATION ALERT: • avoid skin exposure to the drug
• avoid inhaling drug particles
• use special gloves (especially for pregnant women
BLACK BOX WARNING: - DO NOT COMBINE WITH (SELECTIVE - CELECOXIB) NSAIDs ➜ bleeding
- combined with NSAID may cause severe and sometimes FATAL MYELOSUPPRESSION
OVERDOSE TREATMENT: ▪ Leucovorin (folinic acid)
⤷ reduced form of folic acid
⤷ “rescues” normal cells or protect against severe bone marrow damage
⤷ • urine may be alkalinized to protect the kidneys from methotrexate toxicity
IX.
ANTITUMOR ANTIBIOTICS
1. Prototype: doxorubicin (Adriamycin)
2. bleomycin (Blenoxane)
PHARMACOLOGIC CLASS: Antitumor Antibiotics
THERAPEUTIC CLASS: Antineoplastic
♡ ANTITUMOR ANTIBIOTICS: - act by inhibiting cell growth through cytotoxicity (actions similar to alkylating agents)
CARDIOTOXICITY is a major limiting factor
⤷ may occur within minutes or years later
SE: • tachycardia ↑HR, • tachypnea, and/or • dyspnea
AE: CARDIOTOXICITY (irreversible HF)
PROTOTYPE: doxorubicin (Adriamycin) - considered to be one of the most effective single drugs against SOLID TUMORS ROUTE: IV
SE: • ↑HR (tachycardia) • tachypnea, and/or • dyspnea
AE: CARDIOTOXICITY (irreversible HF)
BLACK BOX WARNING: severe myelosuppression may occur
⤷ major dose limiting toxicity with doxorubicin, bone marrow may not make enough blood cells
CONTRAINDICATION: ▪ pregnancy
▪ preexisting cardiac disease (cardiotoxicity)
▪ myelosuppression ▪ lactation
▪ thrombocytopenia
PREGNANCY CATEGORY: D
DRUG-DRUG: St. John’s Wort
ADMINISTRATION ALERT: 1. Extravasation can cause severe pain & extensive tissue damage
⤷ should immediately be treated with local ice pack/ cold compression to reduce absorption of drug
⤷ blood vessels constrict because cold
2. avoid skin contact ⤍ wash with soap & water if exposed
NURSING RESPONSIBILITY: - changes in rectal mucosa contraindicate suppositories or rectal temperature
- wear protective clothing (gloves, mask, & apron) when preparing drug
- monitor IV site ⤍ doxorubicin ⤍ severe vesicant
- give drug through large-bore, quickly running IV (IV site)
- monitor fungal infection (tongue, under skin folds – candiasis)
- monitor cardiovascular status
X.
NATURAL PRODUCTS WITH ANTINEOPLASTIC ACTIVITY
1. Prototype: vincristine (Oncovin) - vinca alkaloid
PHARMACOLOGIC CLASS: Natural Products with Antineoplastic
THERAPEUTIC CLASS: Antineoplastic
INDICATION: • treatment for Hodgkin’s & non-Hodgkin’s lymphomas
• bladder carcinoma, breast carcinoma
• Kaposi sarcoma
• Wilm’s tumor
• leukemia
MOA: kills cancer cells by preventing their ability to complete mitosis
SE: • alopecia
AE: - paresthesia (neurotoxicity) ⇨ numbness & tingling
• constipation
> paralytic ileus ⇨ muscle contraction that moves food through your intestine are temporarily paralyzed
BLACK BOX WARNING: • myelosuppression may be severe & predispose to opportunistic infections
• extravasation can cause intense pain, inflammation, tissue necrosis
PREGNANCY CATEGORY: D
ADMINISTRATION ALERT: 1. extravasation can result in extensive tissue damage [ANYTIME IV GIVEN, EXTRAVASATION IS THE PROBLEM]
⤷ STOP the injection immediately, apply local heat, inject hyaluronidase as ordered
⤷ observe the site for sloughing
⤷ used to ↓ tissue damage in cases of extravasation of drug
2. avoid EYE contact ⤍ severe irritation
OVERDOSE TREATMENT: supportive treatment including administration of leucovorin (folinic acid)
XI.
HORMONES & HORMONE ANTAGONISTS
HORMONES: 1. diethylstilbestrol (DES, Stilbestrol)
2. medroxyprogesterone (Provera, Depo-Provera)
3. megestrol (Megace)
PHARMACOLOGIC CLASS: Hormones & Hormone Antagonists
HORMONE AGONISTS: 1. tamoxifen - estrogen receptor blocker
THERAPEUTIC CLASS: Antineoplastic
▪ GONADAL HORMONES: - used to treat tumor cells that possess specific hormone receptors (ex. breast cancer, prostate cancer)
- produced by androgens, antiandrogens, estrogens, and progestins
♡ Estrogens - diethylstilbestrol (DES, Stilbestrol)
INDICATION: - metastatic breast cancer (Stage IV) and prostate cancer
• the reason why hormone estrogen is used is because it can treat/ block activating estrogen receptors (ERs)
• too much estrogen is being linked to breast cancer – so this is being used
♡ Progestin - medroxyprogesterone (Provera, Depo-Provera) INDICATION: long-term female contraception, each injection prevents ovulation
♡ Progestin - megestrol (Megace) INDICATION: advanced endometrial cancer
PROTOTYPE: tamoxifen - estrogen receptor blocker
INDICATION: • pts. with BREAST CANCER ⤍ stops estrogen dependent cancers
• high-risk pts. to prevent diseases
MOA: blocks estrogen receptors on breast cancer cells
SE: • N/V
AE: ⚬ ↑ risk for thromboembolic events ⤍↑blood clots
• vaginal discharge
• hot flashes, • fluid retention
BLACK BOX WARNING: ↑ risk thromboembolic disease [stroke, PE, DVT]
CONTRAINDICATION: - hx. of thromboembolic disease
- pregnancy, - lactation
PATIENT TEACHING: notice SOB, or swelling in legs, pain, and difficulty walking – NOTIFY MD
PREGNANCY CATEGORY: D
DRUG-DRUG: - anticoagulants concurrently ⤍ ↑risk of bleeding
ADMINISTRATION ALERT: 1. give with food or fluids to ↓ GI irritation
2. DO NOT CRUSH/CHEW DRUG
3. avoid antiacids for 1-2 hours following PO dosage
CHAPTER 39 - DRUGS FOR ALLERGIC RHINITIS & THE COMMON COLD
A. UPPER RESPIRATORY TRACT
a) warms, humidifies, & cleans incoming air
b) nasal mucosa richly supplied with vascular tissue
c) prevents particulate matter & pathogens from getting into bronchioles and alveoli
d) FIRST line of immunologic defense
⤷ • ciliated epithelium
• nasal mucus
• mast cells that line nasal mucosa
B. ALLERGIC RHINITIS - histamine release will cause rhinitis
⤷ runny nose
a) Inflammation nasal mucosa
b) characterized by sneezing, watery eyes, and nasal congestion
c) caused by exposure to antigen (allergen)
d) causes histamine release
e) most common allergens/ causes: ▪ pollen from weeds, grasses, and trees
▪ mold spores, dust mite, certain foods
▪ animal dander
AE: REBOUND NASAL CONGESTION
C. PHARMACOTHERAPY FOR ALLERGIC RHINITIS
Treatment: ⚬ antihistamines
⚬ intranasal corticosteroids
⚬ mast cell stabilizers
⚬ oral and intranasal decongestants
⤷ usually sympathomimetic ➩
[produces physiological effects characteristic of the sympathetic nervous system by
promoting the stimulation of sympathetic nerves]
D. HISTAMINE
⬩ chemical mediator of inflammatory response
⬩ interacts with 2 receptors: - Histamine 1 (H1)
• causes many of the symptoms of allergic rhinitis
XII.
H1-RECEPTOR ANTAGONISTS
1. Prototype: diphenhydramine (Benadryl) ROUTE: PO/ IV PUSH
2. chlorpheniramine (Chlor-Trimeton)
3. clemastine (Tavist)
4. dimenhydrinate (Dramamine)
5. promethazine (Phenergan)
6. cetirizine (Zyrtec)
7. fexofenadine (Allegra)
8. loratadine (Claritin)
PHARMACOLOGIC CLASS: H1-Receptor Antagonists, antihistamine
INDICATION: • treats minor symptoms of allergy & common cold
• tx. vertigo & motion sickness
• mild parkinson’s [tendency to drool a lot. Benadryl is given at later stages to dry out oral secretions not to treat tumors
• insomnia
MOA: histamine (H1) receptor blocker (first generation)
SE: • drowsiness
AE: > occasionally CNS stimulation & excitability
⤷ ANTICHOLINERGIC EFFECTS: • ↑HR, • mild HTN, • dry mouth, • urinary retention
⚬ may cause photosensitivity
⤷ if giving atropine
• constipation
> paralytic ileus
• ↓ UO
> urinary retention (when in sympathetic mode, you don’t pee)
• jittery
> neurotoxicity (numbness, tingling, dizziness)
CONTRAINDICATION: - hypersensitivity to drug
- BPH, ↑ HR
ADMINISTRATION ALERT: ▪ ↑ risk of anaphylactic shock when parentally administered (IV) ⤍ because pushed too fast!
▪ when administering IV ⤍ inject at RATE of 25mg/min - IN 2 MINUTES
⤷ to reduce risk of shock
DRUG-DRUG: - use with CNS depressants with caution such as alcohol or opioids
⤷ ↑ sedation
XIII.
INTRANASAL CORTICOSTEROIDS
1. Prototype: fluticasone (Flonase)
2. beclomethasone (Beconase AQ, Qvar)
3. mometasone (Nasonex)
4. budesonide (Pulmicort)
PHARMACOLOGIC CLASS: Intranasal Corticosteroids
INDICATION: • treat seasonal allergic rhinitis
MOA: ↓ local inflammation in nasal passages ⤍ reduce nasal stuffiness
SE: • nasal irritation, epistaxis (nosebleed)
AE: ⚬ rare
XIV.
ORAL PREPARATION DECONGESTANTS
1. pseudoephedrine (Sudafed) - relive nasal congestion caused by colds, allergies, and hay fever
ROUTE: PO but used to decongest
PHARMACOLOGIC CLASS: Oral Preparation Decongestants
a. more systemic effects
b. response time is slower
c. less effective at relieving severe congestion
d. often combined with antihistamine preparations
*CONTRAINDICATION: HTN
XV.
INTRANASAL DECONGESTANTS
1. Prototype: oxymetazoline (Afrin)
2. Phenylephrine (Afrin, Neo-Synephrine)
PHARMACOLOGIC CLASS: sympathomimetics
THERAPEUTIC CLASS: nasal decongestant
MOA: stimulates alpha-adrenergic receptors in sympathetic nervous system
⤷ - causes arterioles in nasal passages to constrict
- dries mucous membrane
SE: • minor stinging & dryness in nasal mucosa
AE: ⚬ rebound congestion when used for longer than 3-5 days
CONTRAINDICATION: • pts. with HTN }
• diabetes
}
• heart disease } should only use sympathomimetics only on the direction of their healthcare provider
ADMINISTRATION ALERT: - WASH HANDS ⤍ prevent anisocoria (inequality of pupil size) and/or blurred vision
DRUGS TO TREAT COUGH
A. COUGH (BRONCHOSPASM)
a) cough is a natural reflex mechanism
b) serves to forcibly remove excess secretions & foreign material
c) common cold, allergies, asthma can create coughing
B. PHARMACOTHERAPY OF COUGH
MOA: a) Antitussives: used to prevent or relieve cough
b) Opioids: used to inhibit severe cough
c) Expectorants: remove mucous production
d) Mucolytics: loosen bronchial secretions
XVI.
ANTITUSSIVES: OPIOIDS
1. codeine
DRUG: codeine - usually added to promethazine (Phenergan)
⤷ to make a combo COUGH SYRUP
INDICATION: severe cough (esp. when pts. have difficulty sleeping from coughing)
CONTRAINDICATION: - RR < 12
- ↓ BP
- anything that affects RR [valium, ativan, morphine, fentanyl]
XVII.
ANTITUSSIVES: NON-OPIOIDS
1. Prototype: dextromethorphan (Robitussin DM)
2. benzonatate (Tessalon)
PHARMACOLOGIC CLASS: drug for increasing cough threshold
THERAPEUTIC CLASS: cough suppressant
INDICATION: used in most OTC severe cold & flu preparations
MOA: acts on medulla to inhibit cough reflex
SE: • drowsiness
AE: rare
CONTRAINDICATION: • NO treatment of chronic cough due to excessive bronchial secretions (COPD)
⤷ because suppressing the cough reflex is NOT desirable in these pts.
ADMINISTRATION ALERT: - avoid pulmonary irritants (smoking or other fumes)
⤷ ↓ drug effectiveness
- pts. cough is NOT relieved by dextromethorphan (Robitussin DM) after several days of therapy, should notify their HCP
DRUG-DRUG: • alcohol, opioids, other CNS depressants ⤍ result in sedation
• NO GRAPEFRUIT JUICE - can ↑ serum levels of dextromethorphan (Robitussin DM)
⤷ toxicity
XVIII.
EXPECTORANT
1. guaifenesin (Mucinex)
PHARMACOLOGIC CLASS: Expectorant
INDICATION: ▪ cystic fibrosis ▪ chronic bronchitis
▪ other diseases producing thick mucus
MOA: - directly breakdown mucus molecules
- ↓ viscosity/ make mucous thinner
⤷ easy removal by coughing
Expectorants and Mucolytics are the same except for the drug name. It works by thinning and loosening mucus in the airways, helping to clear chest congestion
and making breathing easier.
XIX.
MUCOLYTICS
1. acetylcysteine (Mucomyst)
PHARMACOLOGIC CLASS: Mucolytic
INDICATION: ▪ cystic fibrosis ▪ chronic bronchitis
▪ other diseases producing thick mucus
MOA: - directly breakdown mucus molecules
- ↓ viscosity/ make mucous thinner
⤷ easy removal by coughing
Expectorants and Mucolytics are the same except for the drug name. It works by thinning and loosening mucus in the airways, helping to clear chest congestion
and making breathing easier.
CHAPTER 40 - DRUGS FOR ASTHMA & PULMONARY DISORDER
▫ ASTHMA: inflammation of airways that causes closure – tightening – difficult to get air
▫ BRONCHIAL CONSTRICTION (wheezing)
THERAPEUTIC GOAL: relax smooth muscles (allow bronchodilation)
2 TYPES OF BRONCHODILATOR
• SHORT ACTING BRONCHODILATOR – SABA (rescue drugs): - if you’re having acute onset of broncho constriction these drugs will help relax the smooth
muscle and allow bronchodilation to occur
• LONG ACTING BRONCHODILATOR – LABA (maintenance): - used for long term control of asthma, or other pulmonary disease, COPD,
- Albuterol (ER): not meant to use for acute onset
A. Autonomic Control of Airways
SYMPATHETIC BRANCH
• activates beta 2-adrenergic receptors
& causes bronchiolar smooth muscle to
relax
• the airway diameter increases
⤷ bronchodilation
PARASYMPATHETIC BRANCH
• causes bronchiolar smooth muscles to contract
↓
bronchospasm (cough)
• the airway diameter is narrowed
- bronchoconstriction
- results in less airflow
B. Asthma
a. chronic inflammation disease
b. symptoms occur exposure to triggers or with exertion (exercise induced)
C. Status Asthmaticus
a. acute exacerbation of asthma that does not respond to standard treatments of bronchodilators and corticosteroids
b. Symptoms: - chest tightness
- dry cough
- rapidly progressing fast and/ or labored breathing
- use of accessory respiratory muscles
- extreme wheezing
c. life-threatening episode of airway obstruction • medical emergency
d. complications include cardiac and/or respiratory arrest
D. Goal of Therapy
a. Asthma: bronchoconstriction & inflammation
b. Goal: 1. terminate acute bronchospasms in progress (quick relief medication)
2. reduce the frequency of asthma attacks (long-acting medication)
E. Quick-Relief Medication
CLASS
MECHANISM
USE
1. SABA-short acting beta 2- adrenergic
bronchodilation
• preferred drugs for relief of acute symptoms
2. Anticholinergic
bronchodilation
• alternate drugs for those who cannot tolerate SABAs
3. Corticosteroids: systemic (PO)
Anti-inflammatory
• although not rapid-acting, these oral drugs are used for short periods to reduce the
frequency of acute exacerbation
F. Long Acting Medication
CLASS
1. corticosteroids: inhaled
MECHANISM
Anti-inflammatory
2. mast cell stabilizer
3. leukotriene modifiers
Anti-inflammatory
Anti-inflammatory
4. LABAs: long-acting beta 2-adrenergic
agonists
5. Methylxanthines
bronchodilation
bronchodilation
USE
• preferred drug for long-term asthma management.
oral doses may be required for severe, persistent asthma
• alternative drugs to control mild, persistent asthma or exercise induced asthma
• alternative drugs to control mild, persistent asthma or as adjunctive therapy with
inhaled corticosteroids
• used in combination with inhaled corticosteroid for prophylaxis of moderate –
severe persistent asthma
• used in combination with inhaled corticosteroid for prophylaxis of mild – moderate
persistent asthma
G. Devices used to deliver respiratory drugs
a. meter dosed inhaler
b. nebulizer with mask
c. dry powder inhaler
BETA 2-ADRENERGIC AGONIST: - a class of medications used in the frontline management and treatment of bronchial asthma and COPD.
- cause dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin
- stimulate B2 receptor sites
- used to dilate airways to be easier to breath if you have asthma
- short acting & works quickly
XX.
BETA 2-ADRENERGIC AGONIST – [SHORT ACTING BETA AGONISTS - SABA]
1. Prototype: albuterol (Ventolin) SABA
2. levalbuterol (Xopenex) SABA
3. terbutaline (Brethine) SABA
4. salmetrol (Serevent Diskus) LABA
PHARMACOLOGIC CLASS: Beta 2-Adrenergic Agonist
THERAPEUTIC CLASS: bronchodilator
INDICATION: • SABA used to relieve the bronchospasm of asthma
• rapid onset & excellent safety profile
⤷ PREFERRED drug for termination of acute bronchospasm
• inhaled 15-30 min. prior to physical activity
⤷ prevent exercise induced bronchospasm
MOA: - activates beta 2 receptor sites in bronchial smooth muscles ⇨ bronchodilation
- facilitates mucus drainage & can inhibit the release of inflammatory chemicals from mast cells
SE: • tachycardia ↑HR (↑HR because bronchodilates)
AE: - palpitations
UNCOMMON AE: chest pain
• dry mouth
- headache
• nervousness or restlessness
- insomnia - tremors
• constipation (long term use)
- hypotensive shock (hypotension)
CONTRAINDICATION: • ↑HR
• hx. of cardiac disease or HTN
• coronary artery disease (CAD) - short acting beta agonist contraindicated in SABA
⤷ always a reflection of cardiac ischemia
ADMINISTRATION ALERT: - proper use of the inhaler is important to the effective delivery of the drug (observe & instruct pt. with proper use)
- assess HR prior to administration
- DO NOT ADMINISTER for pt. with hx. of dysrhythmias or MI
- NOT recommended for women who are breastfeeding
DRUG-DRUG: • beta-blocker (nonselective B-blocker)
⤷ inhibit the bronchodilation effects of albuterol (Proventil, Ventolin)
• caffeine ⤍ may ↑ SE of nervousness or palpitations
• NSAIDs ⤍ because hypersensitivity
⤷ broncho constrict which counteracts the albuterol’s broncho dilate
XXI.
ANTICHOLINERGICS
1. Prototype: ipratropium (Atrovent HFA) ROUTE: Intranasal
2. tiotropium (Spiriva)
PHARMACOLOGIC CLASS: Anticholinergics
THERAPEUTIC CLASS: bronchodilator
INDICATION: • relief of acute bronchospasm d/t COPD (bronchitis, emphysema)
• sometimes combined with beta-agonists or glucocorticoids
• prescribed for chronic bronchitis
• symptomatic relief of nasal congestion
MOA: - causes bronchodilation by blocking cholinergic receptors in bronchial smooth muscle
- blocks the parasympathetic nervous system
SE: • bitter taste in mouth (relieved by rinsing mouth after use)
AE: - few AE
• epistaxis (excessive drying of nasal mucosa)
ADMINISTRATION ALERT: - proper use of the inhaler is important to the effective delivery of the drug
- wait 2-3minutes between dosages
- avoid contact with eyes (blurred vision may occur)
- NOT USE FOR ACUTE ASTHMA ATTACK - USED FOR LONG TERM MAINTENANCE OF BRONCHOSPASM ASSOCIATED
WITH COPD
DRUG-DRUG: use with other drugs in this class such as atropine ⤍ addictive anticholinergic SE
⤷ • Drugs with atropine: lomotil/atropen
• Drugs with anticholinergic properties: - benztropine mesylate (Cogentin)
- oxybutynin (Ditropan XL)
- tolterodine (Detrol)
- propantheline (Pro-banthine)
- Seopalamine
XXII.
METHYLXANTHINES
1. theophylline (Theo-Dur) ROUTE: IV or PO
2. aminophylline
- Methylxanthines represent a unique class of drugs for the treatment of asthma.
- Methylxanthines bind to adenosine receptors in the brain resulting in CNS stimulation, which promotes respiratory drive.
- theophylline has demonstrated efficacy in attenuating the three cardinal features of asthma - reversible airflow obstruction, airway hyperresponsiveness, and
airway inflammation
PHARMACOLOGIC CLASS: Methylxanthines
THERAPEUTIC CLASS: bronchodilator
INDICATION: • long term prophylaxis of asthma that is unresponsive to beta agonist or corticosteroids
SE: • N/V ⤍ loss of appetite
• CNS stimulation
• ↑ HR
CONTRAINDICATION: - CAD
- angina pectoris ⤍chest pain
- severe renal or liver disorder
- peptic ulcer
- NOT recommended in women who are breastfeeding
METHYLXANTHINES: a group of bronchodilators related to caffeine
XXIII.
CORTICOSTEROIDS “-ONE”
1. beclomethasone (Beconase AQ, Qvar)
A. General Information
a. most potent natural anti-inflammatory drugs
b. inhaled route ⤍ drugs of choice for long-term prophylaxis of asthma
- must be taken daily (3-4 weeks before optimal benefits are obtained)
- SE: rare
- long-term intranasal/inhaled corticosteroids may cause growth inhibition in children
c. PO ⤍ used for short-term therapy of severe, acute asthma
⤷ limit therapy to under 10 days
♡ PROTOTYPE: beclomethasone (Beconase AQ, Qvar)
PHARMACOLOGIC CLASS: Corticosteroids
INDICATION: • aerosol inhalation ⤍ chronic asthma (Qvar)
• nasal spray ⤍ allergic rhinitis (Beconase)
MOA: - ↓ inflammation (↓ frequency of asthma attack)
- NOT A BRONCHODILATOR (should NOT be used to terminate asthma attacks in progress
SE: • oropharyngeal candidiasis
• ↑ BS
CONTRAINDICATION: - HTN, - HF
*active infection is present because of anti-inflammatory properties
- Cushing syndrome
- fungal infection
- diabetes mellitus
- NOT recommended for pregnant or breastfeeding women
• PEDS pt. - reduce growth velocity in some children
PATIENT TEACHING: • S/S of simple infection (thrush)
• rinse mouth after using steroid inhaler (oropharyngeal candidiasis)
• monitor glucose levels
CORTICOSTEROID TOXICITY: thrush infection, ↑ BS,
XXIV.
MAST CELL STABILIZERS
1. cromolyn (Intal)
PHARMACOLOGIC CLASS: Mast Cell Stabilizers
INDICATION: • alternate drug for milk/ persistent asthma
• exercise induced asthma
XXV.
LEUKOTRIENE MODIFIERS
1. Prototype: montelukast (Singlulair) - not used as rescue meds
PHARMACOLOGIC CLASS: Leukotriene Modifiers
MOA: prevents airway edema and inflammation by blocking leukotriene receptors in airways
INDICATION: • prophylaxis of persistent, chronic asthma, exercise induced
bronchospasm & allergic rhinitis
• only agent in this class that is approved for pediatric use
• take 2 hours prior to activity – if using to prevent exercise induced bronchospasm
SE: • N/V
AE: few
• headache
CONTRAINDICATION: - hepatic failure ← hepatic impairment
THERAPEUTIC CLASS: Antiasthmatics
CHAPTER 12 - CHOLINERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
AUTONOMIC NERVOUS SYSTEM: autonomic nervous system is a component of the peripheral nervous system that regulates involuntary physiologic
processes including heart rate, blood pressure, respiration, digestion, and sexual arousal
CHOLINERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
⤷ Cholinergic & Anticholinergic
⤷ Parasympathetic System
CHOLINERGIC: another word for parasympathetic
DEFINITION
RESPONISBLE NERVOUS
SYSTEM
RESPONDING
NEUROTRANSMITTERS
TYPES
ADRENERGIC RECEPTORS
Adrenergic receptors are autonomic
receptors that bind to adrenaline and
noradrenaline
sympathetic nervous system
CHOLINERGIC RECEPTORS
Cholinergic receptors are autonomic
receptors that bind to acetylcholine
Adrenaline and noradrenaline
Acetylcholine
Alpha and beta receptors
Nicotinic and muscarinic receptors
Parasympathetic nervous system
A. AUTONOMIC NERVOUS SYSTEM
a. controls involuntary responses by influencing organs, glands, and smooth muscle
b. 2 divisions: 1. Sympathetic Division - fight or flight
2. Parasympathetic Division - rest & digest
c. Neurotransmitters of the Autonomic Nervous System
SYMPATHETIC
PARASYMPATHETIC
• Norepinephrine (NE)
• acetylcholine (Ach) } CH12
- CH13
⤷ targets nicotinic receptor sites located at nerve junction sites for BOTH parasympathetic & sympathetic
⤷ target muscarinic receptor sites located on target organ tissues affected by the parasympathetic system
d. Classification of Autonomic Drugs
⤷ based on 2 possible actions affecting the parasympathetic nervous system
1. CHOLINERGICS
▪ stimulates parasympathetic response
▪ parasympathomimetics
▪ fight or flight
▪ cholinesterase
⤷ breaks down Ach – neurotransmitter of the parasympathetic nervous system
▪ cholinesterase inhibitor
⤷ blocks the breakdown of Ach
⤷ system has ↑Ach: ↑ parasympathetic system
2. ANTICHOLINERGICS
▪ known as cholinergic-blocking agents
⤷ inhibits the parasympathetic system – ↑ sympathetic system
• parasympatholytic
B. CHOLINERGIC DRUG - ↑ parasympathetic system
DRUGS
INDICATION
Direct Acting Muscarinic
Receptor Agonists
1. bethanechol (Urecholine)
• urinary retention, glaucoma, Alzheimer’s disease
2. pilocarpine (Isopto Carpine)
• glaucoma
Cholinesterase Inhibitors
1. physostigmine (Antilirium)
• treatment of overdose of anticholinergic toxicity
2. donepezil (Aricept)
• Alzheimer’s disease
3. edrophonium (Tensilon)
• Diagnostic for MG
4. neostigmine (Prostigmine)
• MG, urinary retention
5. pyridostigmine (Mestinon)
• MG
XXVI.
CHOLINERGIC DRUGS: DIRECT ACTING MUSCARINIC RECEPTOR AGONIST
1. Prototype: bethanechol (Urecholine)
PHARMACOLOGIC CLASS: Cholinergic Drugs - Direct Acting Muscarinic Receptor Agonist
INDICATION: • urinary retention
• Alzheimer’s disease • glaucoma
MOA: - activate the parasympathetic nervous system indirectly/ directly
- induce rest/digest response
SE: • ↓HR, ↓BP
AE: > symptomatic bradycardia
• sweating
> risk for aspiration because of salivation
• urinary frequency
• profuse salivation
• ↑ libido
CONTRAINDICATION: - pt. with asthma or ↓ HR should not use this drug
NURSING RESPONSIBILITES: *baseline assessment prior to administration
a. obtain VS: BP, PULSE, and RR before administration and for at least 1hr. after SubQ administration
b. bowel sounds ⤍ because parasympathetic system
c. UO ⤍ ↑UO
d. muscle strength ⤍MG
e. mental status
f. assess pt. ability to swallow ⤍ saliva
PATIENT TEACHING: a. report tremors
f. dizziness
b. palpitations
g. dyspnea
c. urinary retention
h. salivation
d. change in BP
i. sweating
e. abdominal pain
j. extreme fatigue
⤷
potential overdose (signs)
⤶
k. be careful removing positions - orthostatic hypotension
l. report any severe muscle weakness: 1HR = overdose/ cholinergic crises
3HR = underdosage/ drug resistance
m. teach pt., family, or caregiver to notify MD
• SOB
• extreme fatigue
• difficulty with chewing or swallowing occurs ⤍ worsen
ADMINISTRATION ALERTS: • report any severe muscle weakness: 1HR = overdose/ cholinergic crises
3HR = underdosage/ drug resistance
TREATMENT OF OVERDOSE: ATROPINE SULFATE - SubQ injection of atropine sulfate is preferred except in emergencies
⤷ IV route may be used
XXVII.
CHOLINERGIC DRUGS: CHOLINESTERASE INHIBITORS
DRUG
INDICATION
Cholinesterase Inhibitors
1. Prototype: physotigmine
(Antilirium)
2. donepezil (Aricept)
• treatment of overdose of anticholinergic toxicity
3. edrophonium (Tensilon)
• Diagnostic for MG
4. neostigmine (Prostigmine)
• MG, urinary retention
5. pyridostigmine (Mestinon)
• MG
• Alzheimer’s disease
1. Prototype: physotigmine (Antilirium)
2. donepezil (Aricept)
3. edrophonium (Tensilon)
4. neostigmine (Prostigmin)
5. pyridostigmine (Mestinon)
PHARMACOLOGIC CLASS: Cholinergic Drugs - Cholinesterase Inhibitors
C. ANTICHOLINERGIC DRUGS
⤷ ▪ cholinergic blocking agents
▪ anticholinergic drugs inhibit parasympathetic impulses
↑ sympathetic activity
▪ effects: - pupil dilation (mydriasis)
- ↑ HR
- drying grandular secretion (dry mouth)
- relaxing bronchi (good if you’re experiencing asthma)
DRUG
INDICATION
1. atropine (Atropen)
• ↑HR, dilate pupil,
overdose tx for anticholinesterase agents
• asthma & COPD
2. tiotropium (Spiriva)
4. propantheline (Pro-Banthine)
• Parkinson’s disease to control involuntary
movement
• IBS, peptic ulcer disease
5. oxybutynin (Ditropan)
• overactive bladder, urinary incontinence
6. dicyclomine (Bentyl)
• IBS
7. tolterodine (Detrol)
8. ipratropium (Atrovent)
• overactive bladder with symptoms of urge
urinary incontinence, urgency, frequency
• asthma & COPD
DRUG
INDICATION
9. scopolamine (Transderm-Scop)
• motion sickness, adjunct anesthesia
3. benztropine (Cogentin)
XXVIII.
CHOLINERGIC-BLOCKING AGENTS (ANTICHOLINERGICS)
1. Protototype: atropine (Atropen)
2. dicyclomine (Bentyl)
3. oxybutynin (Ditropan)
4. propantheline (Pro-Banthine)
5. tolterodine (Detrol)
PHARMACOLOGIC CLASS: Muscarinic Cholinergic Receptor Blocker
INDICATION: • hypermobility disease of GI tract (diarrhea)
⤷ used to GI motility (sympathetic)
• ↑ HR for pts. with bradycardia ↓HR
• dilate pupils during eye exams
• used to treat bronchodilation in pts. with asthma - RARE now because AE: ↑HR
MOA: occupy muscarinic receptor ⤍ blocks parasympathetic action of Ach
• ↑ sympathetic response • ↑ temp. • ↑ HR
SE: • dry mouth
AE: - kidney problems
• urinary retention
- ↑ HR
• constipation
- risk for heat exhaustion/ heat stroke
• photophobia
CONTRAINDICATION: ▪ glaucoma ⤍ ↑pressure within eye
▪ obstructive disorders of the GI, paralytic ileus, bladder obstruction
▪ cardiac insufficiency ⤍ ↑HR
▪ acute hemorrhage ⤍ HTN ⤍ ↓blood flow to organs
▪ MG ⤍ cholinergic drugs help with MG
▪ BPH ⤍ blocks urine outflow ⤍ ↑urinary retention ⤍ ↓kidney function
PATIENT TEACHING: a. report palpitations, SOB, dizziness, dyspnea, syncope
- older pts.: ↑ drowsiness or ↑ CNS stimulation occurring
⤷ even at usual dose of anticholinergics
b. wear sunglasses - photosensitivity because dilated pupils
c. caution when driving
d. avoid prolonged/ strenuous activity in warm or hot environment
⤷ ex. hot tubs/ extra hot showers (dizziness, pale skin, nausea) ⤍ S/S of heat exhaustion or heat stroke
ADMINISTRATION ALERT/ NURSING RESPONSIBILITIES: ⚬ check for hx. of cardiovascular, cerebrovascular, or respiratory disease, glaucoma,
possibility of pregnancy
⚬ evaluate hepatic & renal function test
⚬ obtain baseline VS, UO, bowel sounds, cardiac rhythm
⚬ encourage drinking water, ice chips, oral rinses (non alcohol based)
⤷ because SE dry mouth
DRUG-DRUG: • SAW PALMETTO - ↑ atropine’s effectiveness with chronic use of herb
⤷ often taken for prostate health, hair loss, maintain libido
TREATMENT OF OVERDOSE: physostigmine (Antilirium)
⤷ cholinergic drug that is an antidote for atropine poisoning
- quickly reverses coma caused by LARGE dose of atropine
CHAPTER 13 - ADRENERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
ADRENERGIC DRUGS AFFECTING THE AUTONOMIC NERVOUS SYSTEM
⤷ Adrenergic Agonist & Adrenergic Antagonist
⤷ Sympathetic System
ADRENERGICS - SYMPATHETIC OUTCOMES
SE: ↑HR, HTN, ↑BS, CONSTIPATION
SYMPATHETIC ACTIVITY: - activated under stress, fight or flight
- ↑ HR, ↑ alertness
- dilation of pupils
- secretion of sweat glands
- dry mouth
- relaxation of bladder
A. CATECHOLAMINES (neurotransmitters of the SNS)
Neurotransmitter of the SNS 1. Natural catecholamines (endogenous ⤍ we make them in our body)
a. norepinephrine
b. epinephrine (Adrenaline)
c. dopamine
2. Synthetic catecholamines (exogenous ⤍ we administer as medication)
a. isoproterenol
b. dobutamine
B. Types of Adrenergic Receptors
NEUROTRANSMITTER
RECEPTOR
LOCATION
RESPONSES
Norepinephrine (adrenergic
agonist)
Alpha 1
all sympathetic target organs, except
heart
• constriction of blood vessels, dilation of
pupils
Alpha 2
presynaptic adrenergic nerve terminal
• inhibits release of norepinephrine
Beta 1
heart & lungs
• ↑HR & ↑ force of contraction,
release renin - regulates BP,
↑BP when BP is low
Beta 2
all sympathetic target organs except
heart
• inhibition of smooth muscles
♥ MEDICATIONS AFFECTING….
1. Alpha 1 receptors treat nasal congestion, hypotension, dilation of pupil for eye exam
2. Alpha 2 receptors treat HTN
3. B1 receptor treats cardiac arrest, HR, shock
4. B2 receptor treats asthma and/or premature-labor contractions
♥ CLASSIFICATION OF AUTONOMIC DRUGS
Adrenergic Agonist
Adrenergic Antagonist
• sympathomimetics
• sympatholytics or adrenergic-blocking agents
• directly stimulates SNS
• inhibits the SNS
⤷ ↑ parasympathetic activity
XXIX.
ADRENERGICS (SYMPATHOMIMETICS)
1. Prototype: phenylephrine (Neo-synephrine)
2. Isoproterenol (Isuprel)
ROUTE: intranasal, ophthalmic, SubQ, IV
PHARMACOLOGIC CLASS: Adrenergics
THERAPEUTIC CLASS: nasal decongestant, mydriatic drug, reverse hypotension
INDICATION: • Intranasal Administration ⤍ - reduces nasal congestion by constricting small blood vessels in the nasal mucosa
• Parenteral Administration ⤍ - reverse acute ↓BP caused by spinal anesthesia or vascular shock, IV must be in ICU setting
↓
• phenylephrine - lacks B agonist activity
↓
⤷ produces few cardiac SE
- longer duration of activity + lack of significant cardiac effects
⤷ phenylephrine > epinephrine or norepinephrine in treating acute hypotension ↓BP
MOA: directly stimulates the SNS
SE: • uncommon ⤍ topically or intranasally
AE: ▪ INTRANANSAL ⤍ - burning of mucosa
- rebound congestion if used for prolonged period
▪ IV ⤍ - severe HTN (because pushed too fast)
- angina/MI - in the presence of CAD
chest pain because lack of O2 to heart muscle hurts ⤶
⤷ because heart is working harder
BLACK BOX WARNING: • IV admin. - severe reaction including death
NURSING RESPONSIBILITIES: ▪ monitor S/S for excessive ANS stimulation: - ↑ BP, ↑ HR [monitor ECG & CO]
▪ monitor diabetes for ↓BS – ↑ glucose from ↑ sympathetic response
▪ EXTRAVASATION: apply cold compress to delay absorption of drug
▪ VASOCONSTRICTOR EXTRAVASATES: apply warm
PATIENT TEACHING: • report palpitations, SOB, chest pain, nervous tremors, ↑ urinary retention
• limit caffeine
• avoid prolonged use nasal spray
XXX.
ADRENERGIC-BLOCKING DRUGS (ANTAGONISTS) [adrenergic blocking agents or sympatholytic]
1. Prototype: prazosin (Minipress)
PHARMACOLOGIC CLASS: Alpha 1-adrenergic blocker/ Antagonist
INDICATION: • tx. of HTN
• management for BPH - relaxes urethral smooth muscle & improves urine flow
MOA: ▪ inhibit symphathetic nervous system
▪ because prazosin (Minipress) is a selective A1 adrenergic antagonist, it competes with norepinephrine at receptor sites on smooth muscles in
arteries & veins (NOT heart)
▪ rapid ↓ in peripheral resistance that ↓ BP
▪ used in combination with other drug like B-blockers or diuretics
⤷ to help with HTN
SE: • ↓ BP, orthostatic hypotension
AE: > hypotensive shock, syncope
- profound hypotension ⤍ 2-6 hours after 1st dose
- reflex tachycardia because rapid ↓ BP
NURSING RESPONSIBILITIES: 1. monitor VS
2. monitor BP - orthostatic hypotension
3. monitor HR - for reflex tachycardia
4. monitor UO
5. don’t administer if low BP (90/60)
ADMINISTRATION ALERTS: • monitor for 1st dose phenomenon
• DO NOT CRUSH XL TABLETS
• DO NOT ABRUPTLY STOP MEDICATION
DRUG-DRUG: ▪ concurrent use of antihypertensives & diuretics } result in ↓ BP
▪ avoid alcohol
▪ avoid SAW PALMETTO
⤷ blocks A1 receptors - dilation of blood vessels & ↓ BP response
TREATMENT OF OVERDOSE: - fluid expanders ⤍ Normal Saline or Lactated Ringer’s
- vasopressors ⤍ dopamine
- stop medicine and give fluff (normal saline) until you get a map of 50-100 systolic then slow it down but don’t stop IV