BVS 611 Slide Deck II

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BVS 611 Slide Deck II
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Which of the following insulin products is a
short-acting insulin? a.) insulin aspart b.)
insulin glargine c.) insulin detemir d.) NPH
insulin Which of the following is a potential
consequence of diabetes-related
gastroparesis? a.) increased risk of myocardial
infarction b.) decreased immunocompetence c.)
speeding up hepatic metabolism of orally-ingested
drugs d.) slowing the absorption of
orally-ingested drugs
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Glyburide (Micronase, DiaBeta) Type-2 diabetes Sulfonylurea agent. Stimulates acute release of insulin from functional beta cells. May increase insulin sensitivity in target cells. Hypoglycemia, wt.gain, hepatic renal complications blood dyscrasias, GI disturbances, headache, increased cardiac risk in those with CV disease. Patient monitored for hepatic and renal function. Doses are reduced in elderly patients. Ocular side effects include blurred vision and changes in accommo-dation. Best effect as monotherapy is approx. 1.5 reduction in A1C. DD intrx c/ some SOP meds
Glipizide (Glucotrol, Glucotrol XL ) Type-2 diabetes Sulfonylurea agent. Stimulates acute release of insulin from functional beta cells. May increase insulin sensitivity in target cells. Hypoglycemia, wt.gain, hepatic renal complications blood dyscrasias, GI disturbances, headache, increased cardiac risk in those with CV disease. Patient monitored for hepatic and renal function. Doses are reduced in elderly patients. Ocular side effects include blurred vision and changes in accommo-dation. Best effect as monotherapy is approx. 1.5 reduction in A1C. DD intrx c/ some SOP meds
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Glimepiride (Amaryl) Type-2 diabetes Sulfonylurea agent. Stimulates acute release of insulin from functional beta cells. May increase insulin sensitivity in target cells. Hypoglycemia, wt.gain, hepatic renal complications blood dyscrasias, GI disturbances, headache, increased cardiac risk in those with CV disease. Patient monitored for hepatic and renal function. Doses are reduced in elderly patients. Ocular side effects include blurred vision and changes in accommo-dation. Best effect as monotherapy is approx. 1.5 reduction in A1C. DD intrx c/ some SOP meds
Acarbose (Precose) Type-2 diabetes Inhibits breakdown of complex starches to glucose, slows absorption of glucose into the bloodstream Flatulence, diarrhea, abdominal pain. Should not cause hypoglycemia when used as monotherapy. If it occurs, treat with oral glucose instead of table sugar (sucrose.) Caution is used when the drug is administered with other medications that lower blood glucose due to increased risk of hypo- glycemia. Best effect as an adjunct is approx. 0.5 0.8 reduction in A1C. Not used as monotherapy.
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Miglitol (Glyset) Type-2 diabetes Inhibits breakdown of complex starches to glucose, slows absorption of glucose into the bloodstream Flatulence, diarrhea, abdominal pain. Should not cause hypoglycemia when used as monotherapy. If it occurs, treat with oral glucose instead of table sugar (sucrose.) Caution is used when the drug is administered with other medications that lower blood glucose due to increased risk of hypo- glycemia. Renal function should be monitored. Best effect as an adjunct is approx. 0.5 0.8 reduction in A1C. Not used as monotherapy.
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Metformin (Glucophage, Glucophage XR, Fortamet) Type-2 diabetes Potentiates the effect of endogenous insulin. May work by decreasing hepatic glucose production and improving insulin sensitivity. N/V/D, flatulence, rash, weakness, headache, hypoglycemia, lactic acidosis, myalgia, blood dyscrasias, chest discomfort, etc. Caution is used when the drug is administered with other medications that lower blood glucose due to increased risk of hypo- glycemia. Renal function should be monitored. The drug may be DCd in renal dysfunction. Medication is held before surgeries and use of contrast media. Best effect is 1 - 2 reduction in A1C. DD intrx c/ some SOP meds
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Pioglitazone (Actos) Type-2 diabetes Decreases insulin resistance at peripheral sites and in the liver. Caution in patients with edema or heart failure due to fluid retention. Avoid in hepatic impairment (liver function should be monitored.) Can cause edema, weight gain, induce CHF, tooth disorders, headache, myalgia, sinusitis, anemia. Can contribute to hypoglycemia when used with other agents that lower blood glucose. Rare reports of decreased visual acuity, macular edema (new onset or worsening.) Best effect is approx. 0.5 -1.4 reduction in A1C. Used for monotherapy and in combination with other medications. DD intrx c/ trimethoprim
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Rosiglitazone (Avandia) Type-2 diabetes Decreases insulin resistance at peripheral sites and in the liver. Caution in patients with edema or heart failure due to fluid retention. Avoid in hepatic impairment (liver function should be monitored.) Can cause edema, weight gain, induce CHF, tooth disorders, headache, myalgia, sinusitis, anemia. Used as monotherapy or in combination with other hypoglycemic agents. Can contribute to hypoglycemia when used with other agents that lower blood glucose. Decreased visual acuity and macular edema have been reported. Best effect is approx. 0.5 -1.4 reduction in A1C. Used for monotherapy and in combination with other medications. DD intrx c/ trimethoprim
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Nateglinide (Starlix) Type-2 diabetes Stimulates the release of insulin from functioning beta cells. Hepatic function impairment can occur. Can cause hypoglycemia, and other adverse effects. Not used as monotherapy in patients inadequately controlled with other diabetes medications. Medications which increase blood glucose levels may lessen the effects of nateglinide. Best effect is approx. 0.5 -1.5 reduction in A1C. Usually used in combination other medications.
Repaglinide (Prandin) Type-2 diabetes Stimulates the release of insulin from functioning beta cells. Hepatic function impairment can occur. Can cause hypoglycemia and many other adverse effects including blood dyscrasias, blood pressure changes, cardiac complications, etc. Not used as monotherapy in patients inadequately controlled with other diabetes medications. Medications which increase blood glucose levels may lessen the effects of repaglinide. Best effect is approx. 0.5 -1.5 reduction in A1C. Usually used in combination other medications.
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Exenatide (Byetta) (New on the market is Liraglutide (Victoza) Type-2 diabetes Glucagon-like peptide to improve pancreatic beta cell response, moderate glucagon secretion and slow gastric emptying. Avoided in patients with renal insufficiency, severe GI disease, or gastroparesis. reports of pancreatitis. Can also cause dizziness, diarrhea, GI upset, headache, GERD, hypoglycemia, etc. Adjunct in the treatment of patients who take metformin, a sulfonylurea, or combination of these meds but who have not achieved adequate control. Not an insulin substitute. Best effect is approx. 1 reduction in A1C. Given subcutaneously
Pramlintide (Symlin) Adjunct in type-1 and type 2 diabetes Slows rate of food absorp tion,modulates gastric empty-ing. Helps prevent post-meal rise in blood glucose and increases satiety. N/V, abdominal pain, arthralgia, cough, headache, hypoglycemia, fatigue, dizziness, etc. Contraindicated in patients with gastroparesis Doses of other diabetes drugs must be adjusted. Best effect is approx. 0.5 reduction in A1C. Given subcutaneously
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BVS 611 Pharmacology I 8.
Medications for Diabetes
Other medications
Drug Use Mechanism of Action Adverse Effects Admin/PK Comments
Sitagliptin (Januvia) New on the market is Saxagliptin (Onglyza) Adjunct in the treatment of type-2 diabetes Inhibits dipeptidyl peptidase (DPP-4), an enzyme that breaks down incretin hormones. Increases in incretins leads to a rise in insulin levels and a corresponding decrease in blood glucose levels. Upper respiratory tract infections, sore throat, diarrhea, N/V, hypoglycemia, weight gain, headache, rash, pancreatitis, etc. Can contribute to hypoglycemia when used with other agents that lower blood glucose, but is used as an adjunct with other medications. It is therefore important to monitor blood glucose levels. Recent reports of pancreatitis associated with CLASS may affect new entrants and use. Best effect is approx. 0.5 -0.8 reduction in A1C.
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BVS 611 Pharmacology I 9. Respiratory
Medications
Drug Use Mechanism of Action ADEs Administration/PK Comments
Albuterol (Ventolin, Proventil) Asthma, COPD, emphysema, etc. ?2 adrenergic receptor agonist causes bronchodilation Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, etc. Onset of action after inhalation lt15 min. PO and INH products available. Duration approx. 4 hours. Drug of choice for acute asthma symptoms and to prevent effort-associated asthma.
Levalbuterol (Xopenex) Asthma, COPD, emphysema, etc. ?2 adrenergic receptor agonist causes bronchodilation Vasodilation, tachycardia, palpitations, tremor, CNS stim.,etc. Can cause atrial fibrillation if used too often in elderly. INH form only. Longer duration of action, best for maintenance. Should only be used every 6 8 hours.
Pirbuterol (Maxair) Asthma, COPD, emphysema, etc. ?2 adrenergic receptor agonist causes bronchodilation Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, etc. INH form only. Duration is 4-6 hours.
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BVS 611 Pharmacology I 9. Respiratory
Medications
Drug Use Mechanism of Action ADEs Administration/PK Comments
Bitolterol (Tornalate) Asthma, COPD, emphysema, etc. ?2 adrenergic receptor agonist causes bronchodilation Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, etc. INH form only. Duration is 4-6 hours.
Salmeterol (Serevent) Maintenance in chronic asthma, COPD, etc. Long acting ?2 adrenergic receptor agonist Vasodilation, tachycardia, palpitations, tremor, CNS stimulation, nasopharyn- gitis, HA, cough, etc. INH form only, duration is 12 hours, so drug is only used twice a day. Not for acute attacks. Advair Diskus is a combination of salmeterol and fluticasone.
Ipratropium (Atrovent) Bronchospasm associated with COPD in adults. Muscarinic antagonist, reverses acetylcholine-induced bronchospasm. Cough, dry mouth and blurred vision can occur. INH form only. Usually used every 6 hours. Caution in narrow angle glaucoma.
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BVS 611 Pharmacology I 9. Respiratory
Medications
Drug Use Mechanism of Action ADEs Admin/PK Comments
Tiotropium (Spiriva) Bronchospasm associated with COPD in adults, maintenance use. Muscarinic antagonist, reverses acetylcholine-induced bronchospasm. Cough, dry mouth, blurred vision can occur. INH form only. Usually used once daily. Caution in narrow angle glaucoma.
Theophylline, aminophylline products Maintenance therapy in moderate severe asthma, no longer first line therapy. Exact mechanism is unknown, may inhibit enzyme which mediates broncho-dilation N/V, headache, insomnia, tachycardia, dizziness, agitation, seizures, etc. Usually given in PO or IV form. Several drugdrug interactions are possible. Avoid use. Rarely used. Not recommended for patients with seizure disorders, CV disease or PUD.
Cromolyn (Intal), Nedocromil (Tilade) Prophylaxis of asthma attacks maintenance therapy only. Mast cell stabilizers prevent release of histamine. Minimal ADEs, throat irritation and unpleasant taste reported. Inhalant form. May take several weeks for full effect to occur. Not effective in treating acute attacks.
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BVS 611 Pharmacology I 9. Respiratory
Medications
Drug Use Mechanism of Action ADEs Admin/PK Comments
Systemic corticosteroids (prednisone , methylprednis-olone, etc.) Acute asthma and COPD exacer-bation Decrease inflammation and edema in respiratory tract, enhance sympathomi-metic bronchodilator activity. Na/water retention, elevate blood glucose levels, can alter electrolytes, GI irritation, CNS effects, can effect WBC count. Several long-term use consequences. PO/IV/IM administra- tion. Adjuncts in acute situations not able to be controlled with bronchodilators alone. Taper as soon as possible to avoid adrenal reliance. Use increases IOP caution in glaucoma cataracts
Flunisolide (Aerobid) Chronic asthma (main-tenance) Decrease inflammation and edema in respiratory tract, enhance sympathomi-metic bronchodilator activity. Usually does not cause systemic corticosteroid effects. Increased risk of oral candidiasis. Some potential for drug interactions. Inhalant form Similar products beclomethasone (QVAR), mometasone (Asmanex), triamcinolone (Azmacort) Use can increase IOP caution in glaucoma cataracts.
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BVS 611 Pharmacology I 9. Respiratory
Medications
Drug Use Mechanism of Action ADEs Admin/PK Comments
Fluticasone (Flovent) Chronic asthma (maintenance) Decrease inflammation and edema in respiratory tract, enhance sympathomi-metic bronchodilator activity. Usually does not cause systemic corticosteroid effects. Increased risk of oral candidiasis. Some potential for drug interactions. INH form Similar to products above. Use can increase IOP caution in glaucoma cataracts.
Montelukast (Singulair), Zafirlukast (Accolate), Zileuton (Zyflo CR) Chronic asthma prevention / maintenance Leukotriene receptor antagonists HA, GI upset. May cause hepatic ADEs. Some drugdrug interactions. New CNS/Psych warnings. PO forms. Montelukast taken once daily, zafirlukast and zileuton taken BID. Watch for increased respiratory infections in elderly patients.
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BVS 611 Pharmacology I 10. Anti-infective
Medications

Introduction to Anti-infectives Microorganisms
are living forms of microscopic or submicroscopic
size. General groups include - Bacteria
(includes Chlamydiae, Rickettsiae, and
Mycoplasma) - Viruses - Fungi -
Protozoa Bacteria are single-celled
microorganisms occurring in many forms, existing
either as free-living organisms, or as parasites
(as in the case of obligate intracellular
parasites such as Chlamydiae.) Bacteria have a
range of biochemical and often pathogenic
properties. Bacteria are generally small, with a
size ranging from 0.2 to 2 microns.
Bacteria are often initially divided into two
general groups based on their response to the
Grams stain procedure Gram Positive


Gram Negative
After the cell sample is fixed, stained, and
washed, the bacterial cell walls retain the
crystal violet dye, or remain stained. These
bacteria have a purple cell wall when viewed
under the microscope.
After the cell sample is fixed, stained, and
washed, the bacterial cell walls do not retain
the crystal violet dye. (They retain the reddish
safranin dye.) These bacteria are decolorized,
and have a light reddish cell wall when viewed
under the microscope.
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BVS 611 Pharmacology I 10. Anti-infective
Medications

Bacteria are not always able to be fully
identified by Grams stain alone. Other special
stains and dyes may be needed to give a
preliminary or final identification of the
bacteria - Acid fast staining (used for
Mycobacteria) is one example. Some bacteria are
not able to be identified by use of the Grams
stain since they do not possess a rigid cell
wall. Such bacteria may be identified on the
basis of rising antibody titers, special
immunofluorescence assays, etc. - Legionella
(i.e. Legionella pneumophilia) -
Rickettsiae (i.e. Rickettsia rickettsiae)
- Chlamydia (i.e. Chlamydia pneumonia, C.
trachomatis, C. psittaci) - Mycoplasma
(i.e. Mycoplasma pneumoniae) The principal
groups of true bacteria are distinguished by
their morphologic shapes when viewed under a
microscope - Cocci Spherical. Examples are
Streptococci, Staphylococci, and Neisseria -
Bacilli Rod-shaped. Examples are E. coli,
Bacillus, and Clostridia - Spirillum Short,
rigid spirals. An example is Vibrio -
Spirochetes Protozoa-like bacteria that are
thin, flexible, motile, and spiral-shaped.
Examples are Borrelia and Treponema -
Fungus-like Bacteria that possess branching
filamentous elements resembling fungal hyphae.
Examples are Mycobacteria, Nocardia, and
Actinomyces
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BVS 611 Pharmacology I 10. Anti-infective
Medications


- Rickettsiae Extremely small parasitic bacteria
once thought to be viruses because their growth
takes place within a host cell. Rickettsiae do
possess a cell wall and other bacterial
elements. Examples are Coxiella, Typhus and
Rickettsia. Not routinely seen on Grams
stain. - Mycoplasma Very small bacteria that
lack a rigid cell wall. Mycoplasma bacteria are
bound by unit membranes, so are not seen on
routine Grams stain. They are usually diagnosed
on the basis of rising antibody titers. An
example is Mycoplasma pneumoniae. - Chlamydia
Smaller than Rickettsiae, these bacteria were
also once thought to be viruses. Chlamydia are
obligate intracellular parasites which do possess
cell walls and ribosomes, but must rely on the
intracellular processes of the host cell to
produce metabolic energy. Not routinely seen on
Grams stain, Chlamydia are often diagnosed using
titers. Examples are Chlamydia pneumoniae, C.
trachomatis, and C. psittaci. - Viruses are
the smallest microorganisms known to have
pathogenic properties in humans. The size of
these microorganisms can be in nanomicrons.
Viruses commonly consist of a nucleic acid
fragment (DNA or RNA) core, a capsid, and a
lipoprotein coat. Viruses generally use the
structures and systems in host cells to replicate
themselves. Viruses most often involved in
causing eye infections include the herpes
viruses, and adenoviruses.
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BVS 611 Pharmacology I 10. Anti-infective
Medications
Terminology Review Along with initial patient
assessment, identification of the pathogen(s) is
critical in determining the most appropriate
therapy for bacterial infection. Visual
appearance/characteristics and laboratory
analysis of specimens are very important.
SPECIMEN COLLECTION Specimens should be
collected with care to prevent inadvertent
contamination. Specimen collection sites should
represent the suspected location of infection.
Specimen amount should be of sufficient size and
numbers. Specimens need to be placed in
appropriate containers, and labeled carefully.
Delivery to the Laboratory should occur
promptly. CULTURE AND SENSITIVITY A test
in which patient specimens are cultured on
appropriate media and incubated. Bacteria which
have grown on the media are directly isolated,
identified, and tested for susceptibility to
different antibiotics. Sensitivity testing may be
done by using the disc method, automated disc
method, or by serial dilution method.


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BVS 611 Pharmacology I 10. Anti-infective
Medications
CULTURES An example A Grams stain reveals
Gram cocci in chains and pairs. On culturing
the bacteria on a blood agar plate,
the following may be seen
Colonies surrounded by greenish zones partially
hemolytic bacteria Alpha hemolytic Streptococci
such as S. viridans, or S. pneumoniae
Colonies surrounded by clear zones fully
hemolytic bacteria Beta hemolytic Streptococci
such as Group A Streptococci
Colonies not surrounded by zones non- hemolytic
bacteria Gamma hemolytic Streptococci such as
Enterococci.
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BVS 611 Pharmacology I 10. Anti-infective
Medications



SENSITIVITY An example
Disc sensitivity testing Discs containing
different antibiotics and/or different
concentrations of antibiotics are placed on a
growth medium that has been colonized with the
cultured bacteria. After incubation, areas of
inhibited bacterial colony growth are assessed.
Wide zones of inhibited (no) growth indicate
antibiotic sensitivity. Areas with minimal growth
inhibition indicate minimal antibiotic
sensitivity. Areas of no growth inhibition
indicate antibiotic resistance.
Other methods of assessing antimicrobial
resistance and sensitivity include serial
dilution testing.
SENSITIVE MINIMALLY
RESISTANT SENSITIVE
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BVS 611 Pharmacology I 10. Anti-infective
Medications


MINIMUM INHIBITORY CONCENTRATION (MIC) The
lowest in-vitro concentration of antibiotic in
solution with a bacterial suspension that
prevents/inhibits growth of the bacteria after an
incubation period. - If the concentration
of antibiotic represented by the MIC can be
achieved in the patients serum by
normal routes of delivery, the bacteria is said
the be sensitive to the antibiotic. -
If the MIC is above the achievable level, or is
within a range that would be toxic to a
patient, then the bacteria is said to be
resistant to the antibiotic. Susceptibility
and resistance are functions of the site of
infection, the bacteria, and the antibiotic being
tested. BROAD SPECTRUM Antibiotics which halt
the growth of, or eradicate many different
bacteria. NARROW SPECTRUM Antibiotics which
are effective for very specific bacteria only.

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BVS 611 Pharmacology I 10. Anti-infective
Medications



BACTERIOCIDAL Antibiotics whose mechanisms of
action usually result in bacterial cell
death. BACTERIOSTATIC Antibiotics whose
mechanism of action usually result in inhibiting
or arresting the growth, development, or
multiplication of the infecting
bacteria. VIRUSTATIC (Virucidal) Not commonly
used terms. Anti-viral is the more common term,
since causing outright pharmacologic eradication
of the infecting virus is sometimes not
possible. Anti-infective Mechanisms of
Action Most anti-infectives work by one or more
of the following mechanisms 1. Inhibition of
cell wall synthesis, cause cell wall lysis
(Penicillins, cephalosporins,
vancomycin, (daptomycin)) 2. Alteration of cell
membrane permeability, inhibition of active
transport across the cell membrane
(Most antifungals) 3. Inhibition of protein
synthesis via inhibition of ribosomal subunit
transcription/translation
(Macrolides/ketolides, tetracyclines,
glycylcyclines, (daptomycin), quinu/dalfo,
aminoglycosides, clindamycin, linezolid) 4.
Inhibition of nucleic acid synthesis/replication,
stimulating reduction products
(Sulfonamides, metronidazole, possibly
tinidazole) 5. Inhibition of DNA-gyrase or
DNA-polymerase (Fluoroquinolones) 6. Binding to
DNA, interfering with/preventing replication
(Most antiviral agents)
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BVS 611 Pharmacology I 10. Anti-infective
Medications

• Considerations in Selecting Appropriate
  Antimicrobial Agents
• 1. The infecting microorgansim and its
  susceptibilities
• 2. The type of infection abscess, UTI, sepsis,
  meningitis, cellulitis, etc.
• 3. Host factors age, current illnesses, immune
  status, renal function, allergies, other
  medications, WBC count, etc.)
• 4. Anti-infectives and their properties dose,
  routes of administration, metabolic properties,
  where the drug is excreted, protein binding,
  tissue penetration capabilities, potential
  toxicities, potential drug interactions,
  therapeutic serum concentration levels, etc.
• 5. Public health considerations hospital and
  community resistance patterns.

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BVS 611 Pharmacology I 10. Anti-infective
Medications
Reminder
Antibiotics are primarily effective against
bacteria. They do not have clinical effect
against viruses. Antibiotics are also not
effective at treating fungal infections.
Antifungal medications are needed to treat these
infections. Some antibiotics also have
anti-protozoal properties and can be used to
treat infections caused by some protozoa.
Final identification and susceptibilities of the
bacteria to anti-infective agents come from
culture and sensitivity testing. Viral
infections are commonly diagnosed empirically,
but special tests such as immunofluorescent
assays or serum titer analysis may be used in
some cases of serious or systemic illness. Most
Common Infections of the Eye Blepharitis
Hordeolum Conjunctivitis (Bacterial and Viral)
Keratitis (Bacterial and Viral) Dacryocystitis
Canaliculitis Endophthalmitis Retinitis
Orbital cellulitis
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BVS 611 Pharmacology I 10. Anti-infective
Medications
Matching infection with the etiology



CONDITION COMMON ETIOLOGY
Blepharitis Staphyloccocus aureus, Staphylococcus epidermidis, seborrhea, dry eye, rosacea
Hordeolum External Staphylococcus aureus Internal (Meibomian glands, can be acute, subacute or chronic) Staphylococcus aureus, MRSA (CA or HA)
Bacterial Conjunctivitis Staphylococcus aureus, N. gonorrheae, C. trachomatis, Streptococcus pneumoniae, Hemophilus influenzae
Viral Conjunctivitis Adenovirus (types 3 and 7 in children and types 8,11, and 19 in adults), Herpes simplex types 1 2
Bacterial Keratitis Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Group A Streptococcus (S. pyogenes), Enterobacteriaceae, Listeria, Hemophilus sp. Mycobacterium chelonae post refractive eye surgery.
Viral Keratitis Herpes simplex types 1 2, Varicella-zoster virus
Fungal Keratitis Aspergillus, Fusarium, Candida
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BVS 611 Pharmacology I 10. Anti-infective
Medications
Matching infection with the etiology



CONDITION ETIOLOGY
Protozoan Keratitis Acanthamoeba sp. (Soft contact lens wearers)
Dacryocystitis Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pneumoniae, Group A Streptococci (S. pyogenes), Hemophilus influenzae
Canaliculitis Actinomyces, Fusobacterium, Nocardia, Candida sp., etc.
Endophthalmitis Staphylococcus epidemidis, Staphylococcus aureus, streptococci (including S. viridans, pneumoniae), P. acnes, enterococci, gram negative rods (Hemophilus influenzae, Bacillus sp.), N. meningitidis, Candida sp.
Retinitis Varicella zoster, Herpes simplex, Cytomegalovirus
Orbital cellulitis Streptococcus pneumoniae, Hemophilus influenzae, Moraxella catarrhalis, Staphylococcus aureus, anaerobes, Group A Streptococci, gram negative rods
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BVS 611 Pharmacology I 10. Anti-infective
Medications



Penicillins MOA Bacteriocidal inhibit
bacterial cell wall synthesis, inhibit bacterial
enzymes which assemble peptidoglycan, activate
autolysis. Uses - Dicloxacillin Effective
against some streptococci and staphylococci.
Many bacteria have acquired resistance,
limiting its usefulness. Does not work against
Pseudomonas. MSSA may respond. MRSA does NOT. Is
available in oral form only. - Amoxicillin
Effective against some streptococci,
staphylococci, and Listeria. Additional
effectiveness against a few gram-negative rods
and cocci. Many bacteria have acquired
resistance. Is available in oral form only. Does
not work against Pseudomonas, MSSA or MRSA. -
Amoxicillin/clavulanate Clavulanate added to
restore effectiveness of amoxicillin against
some bacteria that have acquired resistance.
Used orally for some streptococci and
staphylococci, some gram-negative rods and cocci.
Does not work against Pseudomonas. MSSA may
respond. MRSA does NOT. - Ampicillin Effective
against some streptococci, staphylococci and
Listeria. Does not work against Pseudomonas,
MSSA or MRSA.
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BVS 611 Pharmacology I 10. Anti-infective
Medications



Penicillins Adverse Effects and Other
Information Amoxicillin and amoxicillin/clavulana
te need to be dose- adjusted in patients with
renal impairment. Dicloxacillin may not. Consult
a pharmacist for assistance on renal dose
adjustments if patient reports kidney problems,
renal disease, or renal dialysis on the medical
history. Follow scope of practice
recommendations for duration of therapy and for
referral. Consult a pharmacist or a drug
information center for additional assistance with
recommendations for duration of therapy.
Caution in patients with history of allergy to
penicillins. Take thorough medication histories.
Allergic reactions are a common side effect can
be immediate or delayed and can range from
rashes to anaphylaxis. Monitor patients closely.
GI effects with oral use have included nausea,
vomiting, and diarrhea. CNS effects are rare, but
can include confusion, seizures and
encephalopathy. (More common in high doses, and
in infants/children.) Blood dyscrasias can
occur eosinophilia, thrombocytopenia, rarely
leukopenia, neutropenia.
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BVS 611 Pharmacology I 10. Anti-infective
Medications


Cephalosporins MOA Bacteriocidal inhibit
bacterial cell wall synthesis, inhibit bacterial
enzymes which assemble peptidoglycan. Uses -
Cephalexin and Cefadroxil Effective against
many Gram positive bacteria, not good for Gram
negative bacteria in general. Will not cover
anaerobic bacteria, Pseudomonas, or
Enterococci. Many bacteria have acquired
resistance to these agents. Available in oral
form only. - Cefaclor Generally the same Gram
positive coverage as cephalexin and cefadroxil,
has a little more Gram- negative rod coverage.
Does not cover enterococci or Pseudomonas.
Available in oral form only. Note Cefotetan
has been re-approved in generic form in the
United States. Avoid using or
prescribing this cephalosporin in patients
taking anticoagulants/blood thinners due to
increased risk of bleeding interactions. Adverse
Effects and Other Information Some
cephalosporins may need to be dose adjusted in
patients who have renal impairment.
Consult a pharmacist for assistance on renal
dose adjustments if patients report kidney
problems, renal disease or renal dialysis on
medical history. Other adverse
effects include fatigue, dizziness, vertigo, and
headache. Rash and other manifestations of
allergic responses are common.
Exfoliative dermatitis can rarely occur. Nausea,
vomiting and diarrhea are common.
Hepatic and renal effects may rarely occur.
Blood dyscrasias include eosinophilia,
thrombocytopenia, neutropenia, and leukopenia
can occur.
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BVS 611 Pharmacology I 10. Anti-infective
Medications



Follow scope of practice recommendations for
duration of therapy and for referral. Consult a
pharmacist or drug information center for
additional assistance with recommendations for
duration of therapy. It is estimated that 2-10
of patients who are allergic to penicillin will
also be allergic to cephalosporins. Allergies to
cephalosporins may occur in up to 5 of patients.
Reactions may range from rash to anaphylaxis.
Take careful patient histories.
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BVS 611 Pharmacology I 10. Anti-infective
Medications



Fluoroquinolones MOA Inhibition of bacterial
DNA-gyrase, which interferes with bacterial
reproduction. Effects are often bacteriocidal.
Most are broad spectrum. Indications Some Gram
, many Gram - bacteria. Not good against MRSA,
not generally recommended against Enterococci.
Most do not adequately cover against Bacteroides,
most will cover Chlamydia. Guard against
over-use as bacterial resistances are
increasing! Uses Examples ciprofloxacin,
gatifloxacin, levofloxacin, moxifloxacin,
norfloxacin, and ofloxacin. Most ophthalmic
solutions used in bacterial conjunctivitis will
be used for 7 days. Most solutions used in
corneal ulcers/keratitis will be used for 5 14
days. Newest addition to the group is
besifloxacin (Besivance). Adverse Effects and
Other Information Patients who are allergic to
one fluoroquinolone can easily cross-react with
others. Avoid use in patients with a history of
allergy to any fluoroquinolone. Avoid
over-use of fluoroquinolones for conjunctivitis.
May cause white precipitate of active drug at
the site of epithelial defect that may be
confused with a worsening infection. There are
numerous potential drug interactions, adverse
effects, and cautions with oral use of
fluoroquinolones. In addition, renal dose
adjustments are also needed in patients with
renal impairment or renal disease who take oral
dosage forms. (Not generally needed for
ophthalmic forms.) Ophthalmic forms will be
preferred for treatment in most cases.
37
BVS 611 Pharmacology I 10. Anti-infective
Medications



Fluoroquinolones Cautions (for ophthalmic
preparations) - Use with great
caution if at all in patients with seizure
history. - Can increase photosensitivity
and cause photophobia. - Counsel patients
on potential ophthalmic adverse effects
burning/stinging sensation in the
eye, blurred vision, redness/irritation in the
eye, eye pain, foreign body
sensation, tearing, and/or dry eye. -
Rare but potentially serious side effects can
include severe exfoliative dermatitis,
severe allergic reactions
including anaphylaxis, periocular or facial
edema, dizziness,
etc. - Potential caution in patients taking
blood-thinning medications. Oral
fluoroquinolones may interact with many other
oral medications. Check for potential drug to
drug interactions with oral medications before
prescribing oral quinolones. Sulfonamides MOA
Sulfa antibiotics are structural analogs of PABA
and competitively inhibit the bacterial enzyme
necessary for incorporating PABA into
dihydrofolic acid, the folic acid precursor.
Inhibiting folic acid formation results in the
bacteria not being able to synthesize amino acids
and DNA. Uses Originally broad spectrum
bacteriostatic antibiotics with specific
antibacterial and antiprotozoal activities.
Acquired bacterial resistances have limited use
of this class, although for some uses, this
class of drugs is still somewhat medically
important. SMX/TMP is currently one of the oral
initial agents to consider for CA-MRSA. ODs can
prescribe oral SMX/TMP.
38
BVS 611 Pharmacology I 10. Anti-infective
Medications



Sulfonamides Sulfacetamide sodium ophthalmic
solution (10, 15, 30), and 10 ophthalmic
ointment occasionally used for bacterial
conjunctivitis. Other agents used primarily for
trachoma /chlamydial infections currently.
Topical form not a good option for CA-MRSA.
Sulfisoxazole 4 ophthalmic ointment and 4
ophthalmic solution occasionally used for
bacterial conjunctivitis. Other agents used
primarily for trachoma/chlamydial infections
currently. Topical form not a good option for
CA-MRSA. Adverse Effects and Other Information
Can cause stinging and burning on application.
Allergic reactions are possible. Potential for
cross-reactivity with other sulfa-containing
drugs. Dermatologic reactions can range from
swelling to hives and rash. Severe exfoliative
dermatitis is potentially possible. Products are
incompatible with silver-containing
preparations. Polymyxin and Bacitracin MOA
Polymyxin is a bactericidal agent that works by
binding to cytoplasmic membranes, disrupting the
structure and altering membrane permeability.
Most effects are against sensitive Gram-negative
bacteria. (Polymyxin has no effect against MRSA.)
Bacitracin is a bactericidal agent that works by
binding to bacterial cell membranes and
interfering with cell wall synthesis. Most
effects are against sensitive Gram-positive
bacteria. Uses Both medications have been used
singly, and in combination with other
anti-infectives (i.e. neomycin) for short-term
treatment of external ocular infections caused by
susceptible bacteria. Not for long-term
treatment. Acquired bacterial resistance has
impacted former widespread usage.
39
BVS 611 Pharmacology I 10. Anti-infective
Medications



Polymyxin and Bacitracin Adverse Effects and
Other Information Local adverse effects are
possible. Check previous patient sensitivity
reactions before usage. Tetracyclines MOA
Inhibit bacterial protein synthesis by binding to
the 30-S ribosomal subunit. Bacteriostatic
effects, variable effects against some
Gram-positive bacteria, reliable effects against
systemic Listeria infections. Have effects
against some specific Gram- negative bacteria
including Neisseria meningitidis and Legionella.
Are effective against Mycoplasma, Chlamydia, and
Rickettsia. Some anti-clostridial activity,
though not against C. difficile. Ophthalmic
preparations are no longer available in the
U.S. Uses Oral use should be rare, and
considered for very specific conditions only
(chlamydial inclusion conjunctivitis, trachoma).
The oral tetracycline group includes doxycycline
and tetracycline. Adverse Effects and Other
Information There are many potential adverse
effects and drug interactions possible with use
of tetracycline antibiotics. Doctors of Optometry
should prescribe these medications sparingly and
with caution.
40
BVS 611 Pharmacology I 10. Anti-infective
Medications



Tetracyclines Numerous drug-to-drug and
drug-to-food interactions exist. Pharmacists can
assist in identifying possible
interactions Photosensitivity is common with
these antibiotics. GI effects
antibiotic-associated pseudomembranous colitis,
N/V, abdominal pain, potential pancreatitis,
hepatic effects Allergic reactions are
possible. Cross-sensitivity exists between agents
in the same class. Avoid use in pregnancy and
in children. Should very rarely be considered
in Optometry practice.
41
BVS 611 Pharmacology I 10. Anti-infective
Medications



Macrolides MOA Inhibit protein synthesis by
binding to 50-S ribosomal subunit. Activity
against some Gram- positive bacteria (Group A, B,
C, and G Streptococcus, Streptococcus pneumoniae,
MSSA, and Listeria) although resistance to many
of these bacteria is increasingly a problem.
Some activity against specific Gram-negative
bacteria (N. meningitidis, M.catarrhalis, H.
influenzae, Legionella) Generally very good for
Mycoplasma, Chlamydia, Rickettsia and some
Clostridia (though not C. difficile.) Uses
Current California Optometry regulations specify
azithromycin is limited to the treatment of
eyelid infections and chlamydial disease
manifesting in the eyes. Erythromycin 0.5
ophthalmic ointment is still available for
superficial ocular infections and neonatal
conjunctivitis. Oral clarithromycin and
erythromycin should be dose-adjusted in renal
impairment. Azithromycin does not need to be
dose-adjusted in renal impairment patients.
Contact a pharmacist for assistance with dose
adjustments, or refer patient. Adverse Effects
and Other Information Taken orally or
parenterally, these drugs can cause some
potentially serious side effects - Hepatic
complications such as hepatitis and jaundice -
Renal complications - GI effects can include GI
irritation, nausea, vomiting, and diarrhea -
Ototoxicity may occur - Allergic reactions.
Cross-reactivity between agents in this class is
possible. - Allergic reactions can range from
mild rash to anaphylaxis. Numerous potential
drug-to-drug interactions exist with
erythromycin, clarithromycin and azithromycin.
Check with a pharmacist as needed.Caution in
patients taking blood-thinning medications.
Monitor for the appearance of super-infection
(candidiasis).
42
BVS 611 Pharmacology I 10. Anti-infective
Medications



Aminoglycosides MOA Inhibition of bacterial
protein synthesis by binding principally to 30-S
and 50-S ribosomal subunits. Aminoglycoside
action in bacteria is specifically bacteriocidal,
however since these drugs do cause eventual cell
death through cytoplasmic membrane disruption.
Some limited activity against MSSA, but not
generally used against Gram-positive bacteria.
Used widely for many Gramnegative bacteria.
Little to no activity against atypical bacteria,
no anaerobic effects. Uses Ophthalmic
products include gentamicin 0.3 ointment and
solution, tobramycin 0.3 ointment and solution,
and neomycin (in combination with other
anti-infectives such as polymyxin, bacitracin,
etc. Occasionally used prophylactically, still
used in some bacterial conjunctivitis or
keratitis cases. Some concern for recently
reported bacterial resistances (Streptococcus
pneumoniae, Pseudomonas). Patients who do not
respond quickly need rapid referral. Adverse
Effects and Other Information Local irritation
can occur with ophthalmic use. Caution in
patients with myasthenia gravis as slight
potential for neuromuscular junction blockade
effects can worsen or exacerbate symptoms.
Monitor for appearance of allergic reactions,
swelling of eyelids, face, appearance of rash,
etc. Dermatologic reactions are rare but
possible.
43
BVS 611 Pharmacology I 10. Anti-infective
Medications



Antiviral Agents Trifluridine 1 ophthalmic
solution is indicated for use in Herpes
simplex-related keratitis and keratoconjunctivitis
. It works by incorporating in place of
thymidine into viral DNA, weakening the viral
ability to infect tissue. It is not indicated for
prophylactic use. Trifluridine 1 ophthalmic
solution should be kept refrigerated. Can cause
hyperemia, epithelial keratopathy, increased
intraocular pressure, dry eye, and irritation.
Patients should also be warned that it can cause
burning or stinging on instillation.
Vidarabine 3 ophthalmic ointment is indicated
for use in Herpes simplex-related keratitis and
keratoconjunctivitis. It works by inhibiting
viral DNA polymerase and prevents lengthening or
building of DNA viral chains. It is not indicated
for use in treating infections caused by
adenoviruses. Can cause local hypersensitivity
reactions including itching, redness, foreign
body feeling in the eye, swelling, pain, burning
or other irritation on application. It can also
increase flow of tears. Can cause increased
sensitivity of eyes to light. Recommend
sunglasses and avoiding prolonged exposure to
sunlight. Can be administered with antibiotics
and corticosteroids. Can cause small punctate
defects in the cornea with too-frequent use.
44
BVS 611 Pharmacology I 10. Anti-infective
Medications



Antiviral Agents Oral acyclovir is listed in the
California Optometry scope of practice for
treatment of ophthalmic Herpes zoster. Acyclovir
works by inhibiting DNA replication and
synthesis. Oral acyclovir should not be taken
by patients who are sensitive to valacyclovir.
Cross-sensitivity can occur. Acyclovir can
cause renal failure, and can complicate or worsen
renal function in patients with renal impairment.
Dose adjustments need to be made in renal failure
patients. Consult a pharmacist for assistance, or
refer patient. Encephalopathy/neurotoxicity,
blood dyscrasias, coagulation problems, hepatic
complications, severe skin reactions, visual
changes, GI disturbances, agitation, dizziness,
myalgia, paresthesias, and other side effects are
possible. The drug must be used with caution
and close patient monitoring. Oral doses should
be taken with a full glass of water. Some
potentially serious drugto-drug interactions are
possible. Consult with a pharmacist as needed.
Valacyclovir (Valtrex) is a prodrug for
acyclovir. MOA is the same as acyclovir. Similar
warnings and potential adverse reactions.
Valacyclovir has recently been added to scope of
practice for doctors of optometry in many states.
45
BVS 611 Pharmacology I 10. Anti-infective
Medications



Antiviral Agents Note Corticosteroids can
accelerate the spread of viral infections and are
usually contraindicated in superficial Herpes
simplex virus keratitis. Steroids may be used
concurrently with trifluridine in the treatment
of Herpes simplex stromal infections. In these
cases, trifluridine should be continued for a few
days after the steroid has been
discontinued. Combination Products Corticoster
oid and anti-infective combinations are sometimes
prescribed for steroid-responsive inflammatory
conditions with bacterial infections or risk of
bacterial infections. Anti-infective component
may consist of sulfacetamide sodium,
neomycin/polymyxin, gentamicin, or tobramycin.
Corticosteroid component may consist of
prednisone, hydrocortisone, dexamethasone, or
prednisolone. All combination ophthalmic
solutions should be shaken well prior to
use. Steroid-containing products can increase
intraocular pressure. Select for use, and
monitor patients appropriately.
46
BVS 611 Pharmacology I 10. Anti-infective
Medications

• TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES
• Note
• Anti-infective use and dosage should be adjusted
  as needed on an individual patient basis, taking
  into account indication for use, allergy
  /intolerance status, age, height/weight,
  functional status of metabolic and elimination
  systems (as appropriate),
• C S results, duration of therapy, potential
  for drugdrug interactions and adverse effects.
• 2. Consult a drug information resource, a
  pharmacist, and/or a drug information center as
  needed. Always consult a drug information center
  or pediatrician for pediatric and infant doses,
  and the physician supervising the pregnancy of
  expectant women.
• 3. Trade names listed below reflect ORAL dosage
  forms/products, not ophthalmic products. The
  symbol ? indicates a medication where the
  knowledge of generic name, dose, and comments
  will be evaluated in BVS 611.

DRUG POSSIBLE REGIMEN COMMENTS
Dicloxacillin(Dynapen) (Gen.) ? 125-500mg PO q 6 hr AC Most adult doses range from 250-500mg. Renal dose adjustment needed.
Amoxicillin (Amoxil, others) (Gen.) ? 250mg 1000mg PO T.I.D. Most adult doses range from 250-500mg. Renal dose adjustment needed.
47
BVS 611 Pharmacology I 10. Anti-infective
Medications



TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES
DRUG POSSIBLE REGIMEN COMMENTS
Amoxicillin-clavulanate (Augmentin) (Gen.) ? 500/125 1 tab PO T.I.D. 875/125 1 tab PO B.I.D. XR-1000/625 2 tabs PO B.I.D. Need to clear both renal and hepatic status. Renal dose adjustment needed.
Ampicillin (Principen,others) (Gen.) ? 250mg-500mg PO q 6 hr Renal dose adjustment needed.
Cefadroxil (Duricef) (Gen.) ? 500mg-1000mg PO q 12hr Renal dose adjustment needed.
Cephalexin (Keflex) (Gen.) ? 250mg-500mg PO q 6hr Renal dose adjustment needed.
Cefaclor (Ceclor) (Gen.) ? 250mg-500mg PO q 8hr Renal dose adjustment needed.
Cefprozil (Cefzil) (Gen.) ? 250mg-500mg PO q 12hr Renal dose adjustment needed.
48
BVS 611 Pharmacology I 10. Anti-infective
Medications
TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES


DRUG POSSIBLE REGIMEN COMMENTS
Cefuroxime axetil (Zinacef, Ceftin) (Gen.) ? 125mg-500mg PO q 12hr Most adult doses range from 250-500mg. Renal dose adjustment needed.
Cefdinir (Omnicef) (Gen.) ? 300mg PO q 12 hr or 600mg PO q 24 hr Renal dose adjustment needed.
Clindamycin (Cleocin) (Gen.) ? 150mg-450mg PO q6hr Hard to tolerate, high potential for serious GI ADEs. Hepatic caution as well.
Azithromycin (Z-Pack, Zithromax, Zmax)(Gen.) ? Other strength products preparations available. For Z-Pack 2 x 500mg tabs PO on day 1, then 1 x 250mg tab PO on days 2-5. Dose varies by indication. Hepatic drug clearance.
Erythromycin base and esters (Numerous products preparations available Eryc, E-mycin, EES, etc.) (Gen.) ? 250mg-500mg q 6 hr Dose varies by indication and product formulation. Can be hard to tolerate PO, hepatic and renal clearance.
49
BVS 611 Pharmacology I 10. Anti-infective
Medications



TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES
DRUG POSSIBLE REGIMEN COMMENTS
Clarithromycin (Biaxin) (Gen.) ? 500mg PO q 12hr Renal dose adjustment needed, caution if hepatic problems as well
Doxycycline Vibramycin, Vibra-Tabs, Doryx, others) (Gen.) ? 100mg PO q 12 hr Mostly hepatic clearance.
Tetracycline (Sumycin) (Gen.) ? 250-500mg PO q 6 hr Renal dose adjustment needed.
Ciprofloxacin (Numerous products preparations available.) (Cipro) (Gen.) ? 500mg-750mg PO B.I.D. Renal dose adjustment needed.
Levofloxacin (Levaquin) ? 250mg-750mg PO q 24hr Renal dose adjustment needed.
Moxifloxacin (Avelox) ? 400mg PO q 24hr No renal adjustment needed.
50
BVS 611 Pharmacology I 10. Anti-infective
Medications



TYPICAL ADULT ORAL ANTI-INFECTIVE DOSES
DRUG POSSIBLE REGIMEN COMMENTS
Gemifloxacin (Factive) 320mg PO q 24 hr Renal dose adjustment needed. Very expensive, rarely prescribed for eye infections by O.D.s as less expensive, equally effective therapy is available.
Trimethoprim/sulfamethox-azole (800mg SMX/160mg TMP double strength) (Bactrim DS, Septra DS) (Gen.) ? For CA-MRSA 2 DS tablets PO B.I.D. Renal dose adjustment needed. (Dose varies depending on whether double strength preparation is used.)
Acyclovir (Zovirax) (Gen.) ? 800mg PO 5x per day Renal dose adjustment needed.
Valacyclovir (Valtrex) (Gen.) ? 1000mg PO T.I.D. for VZV keratitis Renal dose adjustment needed.
Famciclovir (Famvir) ? 500mg PO T.I.D. Renal dose adjustment needed.
51
BVS 611 Pharmacology I 10. Anti-infective
Medications
Anti-infective Treatment Summary



BEFORE PRESCRIBING ANY ORAL MEDICATION, CHECK FOR
POTENTIAL DRUG-TO-DRUG INTERACTIONS. COMPARE THE
DRUG THAT YOU ARE CONSIDERING PRESCRIBING WITH
THE OTHER MEDICATIONS ON THE PATIENTS MEDICATION
HISTORY/PROFILE. SEEK THE ASSISTANCE OF THE
PATIENTS PRIMARY MEDICAL DOCTOR AND/OR A
PHARMACIST IF NEEDED TO INTERPRET RELATIVE RISKS
AND FOR OVERALL PATIENT SAFETY.
52
BVS 611 Pharmacology I 11. Antihypertensive
Medications

General Antihypertensive Classes NOTE THAT THERE
ARE MANY DIFFERENT CLASSES AS WELL AS INDIVIDUAL
DRUGS USED FOR THE TREATMENT OF HYPERTENSION.
STUDENTS SHOULD REFER TO THE DRUG INFORMATION
HANDBOOK FOR MORE DETAILS ON INDIVIDUAL AGENTS.
Class Representative Drugs Mechanism of Action Uses Other Information
Centrally acting adrenergic nerve blockers Clonidine (Catapres), Guanabenz (Wytensin), Guanfacine (Tenex), Methyldopa (Aldomet) a2 agonists, decrease sympathetic outflow from brain to lower blood pressure Hypertension Orthostatic hypotension, sedation and other ADEs possible. Blurred vision, conjunctivitis, and dry eyes are possible
Diuretics Several in different classes, see Diuretics section in syllabus See Diuretics section in syllabus Hypertension, edema, CHF Thiazide diuretics currently used as initial medications for hypertension.
53
BVS 611 Pharmacology I 11. Antihypertensive
Medications



General Antihypertensive Classes
Class Representative Drugs Mechanism of Action Uses Other Information
Selective alpha-adrenergic antagonists Prazosin (Minipress), Doxazosin (Cardura), Terazosin (Hytrin), Tamsulosin (Flomax) Competitive blockade of alpha-receptors Hypertension Doxazosin, Terazosin and Tamsulosin are also used for BPH Orthostatic hypotension and other ADEs possible. Vision abnormalities (blurry vision, etc.) and conjunctivitis can occur. Intraoperative floppy iris syndrome possible in patients undergoing cataract surgery.
54
BVS 611 Pharmacology I 11. Antihypertensive
Medications



General Antihypertensive Classes
Class Representative Drugs Mechanism of Action Uses Other Information
Direct vasodilators Hydralazine (Apresoline), Minoxidil (Loniten) Diazoxide (Hyperstat), Nitroprusside (Nipride) Relaxes arterioles, peripheral vasculature, and/or smooth muscles independent of sympathetic effects. Hypertension and other specific uses. Usually reserved for hypertensive crisis, accelerated hypertension, or advanced cases poorly controlled with more than one other class of antihypertensive agent. Hydralazine can cause lacrimation.
55
BVS 611 Pharmacology I 11. Antihypertensive
Medications



General Antihypertensive Classes
Class Representative Drugs Mechanism of Action Uses Other Information
Beta-adrenergic blocking agents Labetalol (Trandate), Carvedilol (Coreg), Propranolol (Inderal), Sotalol (Betapace), Nadolol (Corgard), Metoprolol (Toprol XL, Lopressor), Timolol (Blocadren, Timoptic), Atenolol (Tenormin) Acebutolol (Sectral). Bisoprolol (Zebeta), etc. Competitive blockade of ß-adrenergic receptors. Some agents are specific for ß1 receptors at usual doses, while others have actions on both ß1 and ß2 receptors. Hypertension. Some used also for cardiac arrhythmias, angina pectoris, glaucoma, migraine prophylaxis, MI prevention, CHF maintenance,etc. Many potential ADRs and drugdrug interactions individual agents need to be reviewed carefully when listed on a medication history. Use of these agents can cause dryness or soreness of the eyes, orthostatic hypotension, etc. Non-selective agents and high doses can exacerbate bronchospasm in asthma or COPD patients.
56
BVS 611 Pharmacology I 11. Antihypertensive
Medications



General Antihypertensive Classes
Class Representative Drugs Mechanism of Action Uses Other Information
Calcium channel antagonists Nifedipine (Procardia), Diltiazem (Cardizem), Verapamil (Calan), Isradipine (Dynacirc), Amlodipine (Norvasc) and others Blocks calcium influx during slow channel exchange, dilates peripheral arterioles, some are used for antiarrhythmic properties, also used for angina prophylaxis. Angina prophylaxis, supraventri-cular tachycardia, hypertension Many potential ADRs and drugdrug interactions individual agents need to be reviewed carefully when listed on a medication history. Transient blindness has been reported rarely with nifedipine.
Aldosterone receptor antagonists Spironolactone (Aldactone), Eplerenone (Inspra) Blocks aldosterone binding to specific renal receptors HypertensionCHF, CHF after after MI, edema Can cause hyperkalemia and nephrotoxicity.
57
BVS 611 Pharmacology I 11. Antihypertensive
Medications



General Antihypertensive Classes
Class Representative Drugs Mechanism of Action Uses Other Information
ACE-inhibitors Captopril (Capoten), Lisinopril (Prinivil, Zestril), Enalapril (Vasotec),Ramipril (Altace), Quinapril (Accupril) and others Blocks conversion of angiotensin-I to angiotensin-II (a vasoconstrictor) and suppresses aldosterone, limiting sodium re-uptake in the kidney. HypertensionCHF, MI Can cause hypotension, dizziness, tachycardia, headache, cough, bradykinin accumulation. Many potential ADRs and drugdrug interactions individual agents need to be reviewed carefully when listed on a medication history. Vision changes have rarely been reported.
58
BVS 611 Pharmacology I 11. Antihypertensive
Medications



General Antihypertensive Classes
Class Representative Drugs Mechanism of Action Uses Other Information
Angiotensin receptor blockers (ARBs) Losartan (Cozaar), Valsartan (Diovan), Irbesartan (Avapro), Candesartan (Atacand), Telmisartan (Micardis) and others Blocks angiotensin-II receptor site to control vasoconstriction. Also suppresses aldosterone. Hypertension Hypotension, dizziness, and other ADEs possible. Conjunctivitis and blurred vision have been reported.
59
BVS 611 Pharmacology I 11.
Antihypertensive Medications

TEACHING CASE Patient with Hypertension
Clinical Clues Interventions Notes
Recommendations
A 56 year-old male patient is receiving his
annual eye exam. On the medication history, the
patient indicates that he takes
hydrochlorothiazide 25mg PO once daily, and that
his physician added metoprolol 50mg PO B.I.D. to
his regimen three months ago. The only vision
complaint that the patient reports since his last
visit to the Optometry office is dry eyes.
The patients blood pressure in the office is
130/86. Should the O.D. report this finding to
the patients physician? What is the pulse
pressure differential based on this blood
pressure reading?
44
Can either of these medications cause or
exacerbate dryness of the eyes?
Metoprolol, like all beta-adrenergic antagonists
(or beta blockers can cause dry eyes as an
occasional side effect. The hydrochlorothiazide
is a diuretic often used as first-line treatment
of hypertension. Being a diuretic, it can
theoretically contribute to dry eyes if the
patient becomes dehydrated.
Since the blood pressure appears to be coming
under better control with the new regimen, the
O.D. could recommend artificial tears to
alleviate dryness of the eyes.
60
This drug is prescribed for oral use by persons
with Type 2 diabetes. It works by decreasing
insulin resistance at peripheral sites and in the
liver, but its best effect will result in a 0.5
1.4 reduction in hemoglobin A1c levels. The drug
has also been associated with rare reports of
causing decreased visual acuity and macular
edema. This description best fits which of the
following medications? a.) metformin
(Glucophage) b.) pioglitazone (Actos) c.)
insulin aspart (Novolog) d.) pramlintide
(Symlin)
A 52 year-old male patient who is new to an
optometrists practice reports that losartan
(Cozaar) is currently being taken. For which of
the following conditions is this medication MOST
likely prescribed? a.) benign prostatic
hyperplasia b.) hyperthyroidism c.)
hypertension d.) angina
61
Which of the following dosage regimens would be
APPROPRIATE when prescribing oral acyclovir
(Zovirax) in an adult patient with no known
allergi