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Antibiotics

1. Penicillins-(beta-lactam class, narrow, extended spectrum)-inhibitors of cell wall synthesis,


bactericidal.
2. Cephalosporins - (beta-lactam class, extended spectrum) - inhibitors of cell wall synthesis,
bactericidal.
3. Sulfonamides - inhibitors of other metabolic processes or folate pathway inhibitors,
bacteriostatic.
4. Macrolides - inhibit protein synthesis in susceptible bacteria (RNA), bacteriostatic, may be
bactericidal.
5. Tetracyclines - inhibitors of protein synthesis, bacteriostatic.
6. Beta-Lactams - A broad and widely used class of bactericidal antibiotics, consisting of all
antibiotic agents that contains a β-lactam ring in the molecular structure.
7. Glycopeptides-(Vancomycin, Fosfomycin)- inhibit cell wall synthesis at a site different
than the beta-lactams, bactericidal.
8. Aminoglycosides - inhibitors of protein synthesis, bactericidal
9. Quinolones/ Fluoroquinolone - inhibitors of nucleic acid (DNA) synthesis, bacteriostatic,
may be bactericidal, used for gram negative and gram positive bacteria, mild to the kidney.
Antivirals
1. Nucleoside analogs - Act by inhibiting enzyme that is needed to put together the building
blocks of viral DNA (purines, pyrimidines) and acts on DNA polymerase = interference with
DNA synthesis and impairs viral replication.
2. Acyclovir – treat Herpes Simplex Virus (HSV)-1,2, and Varicella Zoster Virus(VZV)-
Chicken pox or Shingles, IV and PO.
3. Famciclovir- treat Herpes Simplex Virus (HSV)-1,2, and Varicella Zoster Virus(VZV) )-
Chicken pox or Shingles, IV and PO.
4. Ganciclovir – Cytomegalovirus(CMV) infections (treatment and prophylaxis), IV and PO.
5. Ribavirin - Cytomegalovirus(CMV) infections (treatment and prophylaxis) IV and PO.
6. Amantadine - early anti-viral, influenza A, can used to prevent or treat, Post Exposure
Prophylaxis (PEP), PO.
7. Oseltamivir- (Tamiflu)/Zanamivir- newer, influenza A and B, prevent or treat (started with
2 days of exposure), Post Exposure Prophylaxis PEP, PO.
HAART /ART - (Highly Active Anti-Retroviral Therapy)
FUSION/ENTRY INHIBITORS
1. Enfuvirtide (Fuzeon) - Fusion inhibitor -Stops or block the fusion of HIV to CD4 (T-cells)
receptors on the lymphocytes, given only by injection.
2. Maraviroc - (Entry inhibitor) - Prevents HIV from entering healthy cells and inserting its
genes.
REVERSE TRANSCRITASE INHIBITORS
3. Zidovudine(AZT), Tenofovir disoproxil (Viread) - Reverse transcriptase is an enzyme that
is makes DNA out of HIV RNA, transcriptase inhibitors block reverse transcription, and
these drugs are “analogues” trick the virus into taking them instead of host cells molecules.
4. Nevirapine (Viramune) - Reverse transcriptase is an enzyme that is makes DNA out of HIV
RNA, transcriptase inhibitors block reverse transcription, and these drugs are “analogues”
trick the virus into taking them instead of host cells molecules.
INTEGRASE INHIBITORS
5. Raltegravir - helps block integration of HIV DNA into cell nucleus. Raltegravir (Isentress)
(only one currently available).
PROTEASE INHIBITORS
6. Indinavir sulfate (Crixivan)- breaks down the amino acid structure of protein molecules
into smaller molecules to build future viruses, interferes with protease enzyme, thereby
causing assembly of non-functional virions(decrease infections), and slows the progression
of HIV (best given on empty stomach).
7. Saquinavir(Invirase) - breaks down the amino acid structure of protein molecules into
smaller molecules to build future viruses, interferes with protease enzyme, thereby causing
assembly of non-functional virions(decrease infections), and slows the progression of HIV
(best given on empty stomach).
8. Nelfinavir(Viracept) - breaks down the amino acid structure of protein molecules into
smaller molecules to build future viruses, interferes with protease enzyme, thereby causing
assembly of non-functional virions (decrease infections), and slows the progression of HIV
(best given on empty stomach).

Antifungals
1. Polyene - Binds to ergosterol (main sterol in fungal cell membrane i.e., cholesterol in
humans) in fungal cell membrane creating channels that allow potassium and magnesium
ions to leak out of the cell and this interferes with cell metabolism and leads to cell death.
• Amphotericin B – IV- broad spectrum of severe systemic fungal infections.
• Nystatin - PO/ topical infections only (skin, oral, vaginal).
2. Imidazoles (ketonazole)- (“azole” family of anti-fungal, The “holes” punchers) - creates
“holes” in fungal cell membrane by inhibiting the P450enzyme needed to produce ergosterol
causing a different sterol to be made, causing electrolyte leakage and interferes with cell
metabolism, causing cell death.
3. Triazole (fluconazole-(Diflucan) – given PO or IV, itraconazole, voriconazole,
posaconazole- (“azole” family of anti-fungal, The “holes” punchers ) - creates “holes” in
fungal cell membrane by inhibiting the P450enzyme needed to produce ergosterol causing a
different sterol to be made, causing electrolyte leakage and interferes with cell metabolism,
causing cell death.
• Fluconazole- crosses into CSF and used in treatment of cryptococcal meningitis. Less
side effects and for rapidly growing fungi.
• Itraconazole - widely distributed, useful in immunocompromised clients, nail fungus.
4. Echinocandins) - Prevent the synthesis of glucans (an essential fungal cell wall component)
leading to cell death.
• Capsofungin (micafungin, anidulafungin) - IV treatment of severe Aspergillus
infections or infections that do not response to other drugs. Caution in clients with liver
impairment
Cholinergic drugs - Direct
Parasympathomimetic, cholinergic, cholinergic agonists. Act by stimulating or mimicking the
endogenous neurotransmitters (Ach) in the PNS.
1. Bethanechol (Duvoid, Urecholine) Direct acting - useful for urinary retention- Stimulates
smooth muscle contraction of bladder and relaxation of bladder sphincter. PO is preferred
route, may be given SC with caution, 10-50 mg.
• Secondary uses: neurogenic atony of the bladder with retention, treatment of
constipation.
• Other direct acting meds - used topically for increased ocular pressure in glaucoma-
pilocarpine.

Antidote for overdose of a cholinergic drug is Atropine (anticholinergic)

Cholinergic drugs – Indirect


Cholinergics that Block Enzymes (indirect). Also called Cholinesterase inhibitors. Stimulate
primarily muscarinic receptors with the PNS.
2. Edrophonium - (Tensilon, Enlon)- used to diagnose myasthenia gravis.
3. Pyridostigmine (Mestinon) - used for management of myasthenia gravis due to longer effect.
4. Neostigmine - (Prostigmin)- used in the treatment of myasthenia gravis, reversal of
neuromuscular blocking agents post-op.
5. Physostigmine - antidote to counteract anticholinergic drug overdose, organic poisoning.
- controlled by special access program-severe side effects.
Cholinergic drugs - (Indirect) - Role in Alzheimer's Disease, typically used for mild-moderate
disease.
6. Donepezil (Aricept), Galantamine (Reminyl), Rivastigmine (Exelon)- central acting
AChE inhibitor, increases ACh levels. Mainly for mild to moderate disease. Goal of drug
therapy: Slow memory loss, preserve intellectual and emotional function and Improve
ability to function in daily activities.
7. Galantamine- central acting AChE inhibitor, increases ACh levels. Mainly for mild to
moderate disease. Goal of drug therapy: Slow memory loss, preserve intellectual and
emotional function and Improve ability to function in daily activities.
8. Rivastigmine- central acting AChE inhibitor, increases ACh levels. Mainly for mild to
moderate disease. Goal of drug therapy: Slow memory loss, preserve intellectual and
emotional function and Improve ability to function in daily activities.

Cholinergic Overdose- S.L.U.D.G.E. : Salivation, Lacrimation, Urinary incontinence,


Diarrhea, GI cramps, Emesis. Reversal agent: Atropine.
Anticholinergic drugs
Parasympatholytics, cholinergic blockers, anti-cholinergics or antimuscarinics. Block action
of ACh at muscarinic receptors in the PNS. Interact with muscarinic cholinergic receptors, only
at high doses with nicotinic receptors. Mechanism of action: Block or compete for ACh
receptors in target organs in the PNS. Decrease or block PNS response and potentially allows
SNS to be unopposed.

1. Atropine - bradycardia, cardiac arrest, certain eye conditions, cholinergic overdose, or


poisoning.
2. Scopolamine - aka- Jimson Weed–preop sections, palliative care secretion mgt, motion
sickness.
3. Ipratropium(Atrovent) - asthma, COPD
4. Tiotropium (Spiriva)- asthma, COPD
5. Glycopyrrolate - pre-op secretion control
6. Benztropine(Cogentin) -Parkinson's
7. Dicyclomine (Bentyol)- IBS
8. Tolterodine (Detrol &Detrol LA) - overactive bladder
9. Oxybutynin – neurogenic bladder

Antidote for Anticholinergic drugs – Pyridostigmine (cholinergic)

Anti – Parkinson’s Agents


Goal of Therapy :To increase or enhance the action of dopamine in the brain (with
dopaminergic agents) and inhibit the action of ACh (with anticholinergic agents) thus, restoring
the balance between dopamine and Ach.
Dopaminergic drugs - dopamine cannot cross the blood-brain barrier so other drugs that act
like dopamine or increase dopamine concentration indirectly are used. Exogenous dopamine
replaces lost dopamine or enhances what remains.
1. Levodopa (L-dopa) - mainstay of treatment, chemical precursor to dopamine, the precursor
crosses the Blood Brain barrier whereas dopamine cannot. Once in the neurons the precursor
is transformed to active dopamine by dopa-decarboxylase (DDC).
2. Levodopa + Carbidopa - some L-Dopa is broken down in the GI tract and peripheral
tissues before it can reach the brain. Carbidopa inhibits the breakdown of levodopa in GI
tract and peripheral tissue and increases the effect in the CNS. Dosing example: Sinemet
100/25 four times daily.
3. Amantadine - Amantadine (Symmetrel) - Dopamine modulator (indirect-acting) - acts
by releasing dopamine from storage and blocking re-uptake of dopamine therefore
increasing levels available. Some anticholinergic effects. Secondary: relief of drug induced
EPS, influenza A virus PEP.
4. Bromocriptine - direct-Acting Dopamine Receptor Agonist (Ergot) - directly stimulates
dopamine receptors to produce more dopamine. Using these drugs can delay start of
levodopa treatment and/or lessen the dose. Often used after amantadine fails.
Contraindication: adrenergic drugs.
Seizure Medications
Goals of Anti-Seizure Medication
To prevent and control most seizures. To limit firing of neurons and control the spread of
impulses from the firing neurons. To achieve this goal medication/treatment regimen is
individualized to each client. Approx. 70% can become seizure free.
Action of Anti-Epileptics General action
• Stabilize nerve membranes by blocking channels in the cell membrane or altering receptor
sites.
• Alter the movement of electrolytes in cells: Na+, K+, Ca++
• Shift in distribution of ions causes membranes to become less responsive.
• Decreased responsiveness = decreased nerve impulses - increased threshold of brain activity.
• Reduce the neuron response to incoming (sensory) stimuli.
• Decrease or suppress the transmission of one neuron to another

Generalized Seizures
1. Barbiturates – (Phenobarbital and Mephobarbital) - first line treatment for status epilepticus
(less common for seizure prevention). It inhibits conduction of nerve impulses by increasing
action of GABA and this stabilizes nerve membranes and decreases excitability, depresses
impulse conduction to the cerebral cortex, motor areas and cerebellum which decrease motor
output. Longest ½ life of all drugs so once a day dosing.
2. Hydantoins - Phenytoin (Dilantin), Fosphenytoin (Cerebyx) - first line prevention of tonic-
clonic, focal seizures. Act on cell membrane of neurons in the cortex of the brain, affect
Na++, prevents rapid or repeated depolarization & repolarization.
3. Benzodiazepines - Diazepam (Valium), Lorazepam (Ativan), Midazolam (Versed),
Clonazepam (Klonopin) - first line for Status Epilepticus. Many other uses - May potentiate
the effect of GABA and stabilize nerve cell membranes. Short, intermediate, and long acting.
4. Oxazolidinediones (Tridione, Paradione) - absence seizures. Not widely used.
5. Valproic Acid & Divalproex (Derivative) - increases or enhances the brain levels of the
inhibitory neurotransmitter GABA by blocking reuptake. Used for generalized, absence,
myoclonic and focal seizures. Also used for bi-polar manic episodes, behavior management
in Alzheimer's. Hepatotoxic. Give with food.
6. Iminostilbenes, Carbamazepine (Tegretol) - second most prescribed, used for focal and
tonic-clonic seizures. Also used for bi-polar, trigeminal neuralgia.
7. Succinimides: Ethosuximide (Zarontin), Methsuximide - first choice in treatment of absence
seizures. Depress the cortex of the brain and raise the seizure threshold.
Miscellaneous
8. Lamotrigine (Lamictal) - used for focal seizures, newer use for tonic-clonic. Also used for
bipolar disorder. Adverse effect: Steven Johnson esp. when taken with Valproic Acid.
9. Gabapentin (Neurontin) - mechanism unknown, similar effects of GABA. Adjunct treatment
of focal seizures. Also used for neuropathic pain.
Muscle Relaxants (Amphetamines & Related Drugs)
Most muscle relaxants relieve symptoms of stiffness and rigidity from muscular injury. Thought
to work by depressing CNS activity.
Amphetamines
Increase the activity of NE and dopamine by increasing their release and blocking reuptake and
inhibiting the enzyme (monoamine oxidase -MAO) that metabolizes catecholamines and results
in stimulation of mental alertness areas of brain (cortex, thalamus).
1. Methylphenidate (Ritalin) - commonly used for ADHD and narcolepsy. Should only be
used for short-term treatment of ADHD. Recommended for≥6 yr.-old ADHD 5mg BID.
Safety for ≤ 3yr. old not established.
Similar Drugs
2. Dextroamphetamine (Dexedrine) -potent appetite suppressant
3. Amphetamine aspartate monohydrate (Adderall)

RELATED DRUGS (Non-Stimulants)


Nonamphetamine stimulants- These are Not controlled substances.
1. Modafinil (Pro vigil, Alertec) - used for narcolepsy (a new drug), unknown mechanism of
action. Promotes wakefulness with less SNS effects.
2. Atomoxetine (Strattera) - used for ADHD. Mechanism unknown but the drug is classified
as a NE reuptake inhibitor. Clients on this drug show improved ability to focus and reduced
hyperactivity.

Key Terms – Antivirals


1. Acquired immunodeficiency syndrome (AIDS) - a chronic, potentially life-threatening
condition caused by the human immunodeficiency virus (HIV).
2. Antibodies - are proteins developed by the body in response to an infection or after
vaccination.
3. Antigen - any molecule, molecular structure, that can bind to a specific antibody or T-cell
receptor. The presence of antigens in the body may trigger an immune response. Antigens
can be proteins, peptides, polysaccharides, lipids, or nucleic acids.
4. Antiretroviral drugs - are treatment of people infected with human immunodeficiency virus
(HIV) using anti-HIV drugs. The standard treatment consists of a combination of drugs (often
called "highly active antiretroviral therapy" or HAART) that suppress HIV replication.
5. Antiviral drugs - are medications that help your body fight off certain viruses that can cause
disease. Antiviral drugs are also preventive.
6. Cell-mediated immunity (CMI) - is an immune response that does not involve antibodies
but rather involves the activation of macrophages and NK-cells, the production of antigen-
specific cytotoxic T-lymphocytes, and the release of various cytokines in response to an
antigen.
7. Deoxyribonucleic acid (DNA) - is the molecule that carries genetic information for the
development and functioning of an organism.
8. Fusion - the merging or coherence of adjacent parts or bodies.
9. Genome - the complete set of DNA (genetic material) in an organism.
10. Herpesviruses - they are known as the human herpesviruses and are herpes simplex virus
type 1, herpes simplex virus type 2, varicella-zoster virus, cytomegalovirus, Epstein.
11. Host - an animal or plant on or in which a parasite or commensal organism lives.
12. Human immunodeficiency virus (HIV) - a virus that attacks the body's immune system. If
HIV is not treated, it can lead to AIDS (acquired immunodeficiency syndrome). There is
currently no effective cure. Once people get HIV, they have it for life. But with proper
medical care, HIV can be controlled.
13. Humoral immunity - The humoral immune response is mediated by antibody molecules that
are secreted by plasma cells. Antigen that binds to the B-cell antigen receptor signals B cells
and is, at the same time, internalized and processed into peptides that activate armed helper
cells.
14. Immunoglobulins - any of a class of proteins present in the serum and cells of the immune
system, which function as antibodies.
15. Influenza viruses - are members of the family Orthomyxoviridae. This family represents
enveloped viruses the genome of which consists of segmented negative-sense single-strand
RNA segments.
16. Nucleic acids - a complex organic substance present in living cells, especially DNA or RNA,
whose molecules consist of many nucleotides linked in a long chain.
17. Nucleoside - a compound (e.g., adenosine or cytidine) commonly found in DNA or RNA,
consisting of a purine or pyrimidine base linked to a sugar.
18. Opportunistic infections - an infection caused by an organism that does not normally cause
disease. Opportunistic infections occur in people with weakened immune systems.
19. Protease - an enzyme which breaks down proteins and peptides.
20. Replication - the action of copying or reproducing something.
21. Retroviruses - any of a family of RNA viruses that have an enzyme (reverse transcriptase)
capable of making a complementary DNA copy of the viral RNA, which then is integrated
into a host cell’s DNA. The family includes a number of significant pathogens, typically
causing tumors or affecting the function of the immune system, e.g., HIV.
22. Reverse transcriptase - also known as RNA-dependent DNA polymerase, is a DNA
polymerase enzyme that transcribes single-stranded RNA into DNA.
23. Ribonucleic acid (RNA) - is a nucleic acid present in all living cells that has structural
similarities to DNA. Unlike DNA, however, RNA is most often single-stranded. An RNA
molecule has a backbone made of alternating phosphate groups and the sugar ribose, rather
than the deoxyribose found in DNA.
24. Virion - an entire virus particle, consisting of an outer protein shell called a capsid and an
inner core of nucleic acid (either ribonucleic or deoxyribonucleic acid—RNA or DNA).
25. Viruses - an infective agent that typically consists of a nucleic acid molecule in a protein
coat, is too small to be seen by light microscopy, and is able to multiply only within the living
cells of a host., e.g., "the hepatitis B virus".

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