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Transcript elevated blood glucose
The Endocrine System
A “communication”
system for the body
Major components of
the endocrine system
are:
Hypothalamus
Pituitary gland
1
The Endocrine System (cont.)
Secondary components of the endocrine system
are:
Thyroid
Parathyroid
Pancreas
Adrenal glands
Gonads
The pituitary gland controls the secondary
components of the endocrine system
2
The Hypothalamus and Pituitary
Gland
Hypothalamus
Controls the activity of the pituitary gland
Pituitary gland
About the size of a large pea
Called the “master gland” because it controls many other
glands
Secretes a number of hormones
Hormones—chemical substances that regulate
certain bodily functions
Steroids—slow acting, long lasting, and usually end in
the suffix “-rone” (examples: testosterone, progesterone)
Peptides and amines—made of proteins, fast acting, and
short lived (examples: insulin, ADH)
3
Female Sex Hormones
Estrogen—responsible for:
Development of secondary sex characteristics
Inhibition of osteoclasts
Bone loss
Progesterone—prepares lining of uterus for
implantation of fertilized egg
4
Female hormones Drug Products
MOA: replaces estradiol in females
Indications: menopausal Sx, prevent osteoporosis,
Generic
Brand
Indications
Conjugated Estrogens
Premarin ®
Hormone
replacement
Ethinyl Estradiol
Estinyl®
Hormone
replacement
5
Oral Contraceptives
Drugs that contain high doses of estradiol and/or progestins
MOA: high levels of hormones “tricks” the body to think its pregnant
and ovulation don’t occurs
Indication: Birth control, vaginal bleeding control, endometriosis
Federal law mandates that the patient package insert be dispensed with
Rx to patient in retail
OC are contraindicated in women with a history of TE disorders,
strokes and breast cancer
DepoProvera is an IM injection used for birth control that lasts for 3
months
Levonorgestrel is available as Plan B, or Next Step.
Take 1 tab as soon as possible after sex and 1 tablet 12 hours later
Generic
Brand (dose forms)
Ethinyl estradiolnorgestimate
Ortho Tri Cyclen (tablet)
EE- norgestrel
Lo-Ovral
EE-norethindrone
Loestrin, Ortho Novum
EE-etonogestrel
NuvaRing (vaginal ring)
EE-norelgestromin
Ortho Evra (patch)
Male Sex Hormone Drug Products
MOA: replaces testosterone levels in men
Generic
Brand(s)
Testosterone
Androgel®, Androderm® and as testosterone
cypionate (IM injection)
Nandrolone
Durabolin ®
Fluoxymesterone
Halotestin®
Oxymetholone
Anadrol®
Side effects: weight gain, muscle hypertrophy, viriziling effects,
priapism, hepatitis and blood filled cysts in liver (oral more than IM),
long term use results in sexual problems, gynecomastia
Because of abuse in sports, federal schedule 3
7
Diabetes Mellitus
A disorder of carbohydrate metabolism
Type I DM
Genetic factors involved
Involves destruction of pancreas by the immune system
Begins as children and young adults
Patients are described as insulinopenic (i.e pancreas
secretes almost no insulin)
Patients are described as thin
Blood abnormalities includes high blood glucose, high
triglycerides level (VLDL), high blood levels of ketone
Physical signs are extreme thirst, nocturia, hypertension
and possible kidney disease.
8
Type II Diabetes Mellitus
Genetic factors involved
Environmental factors involved
Involves the resistance of the body to the hormone,
Insulin.
Also described as Insulin resistance syndrome
Signs and symptoms include those of Type I DM
Metabolic Syndrome or Syndrome X
Independent risk factor for cardiovascular disease
Seen in men and women
Biochemically marked by high blood glucose, cholesterol,
trigycerides
BMI>25
Hypertension of greater than 130 mmHg systolic
Waistline of more than 40 in in men; 35 in in women
9
Therapy of Diabetes
Insulin
MOA: binds to insulin receptor which promotes uptake of
glucose into muscle cells, adipocytes and other cells
Regular insulin or short acting insulin
Humulin ® R or Novolin ®R
Humalog ® (Insulin lispro) or Novolog ® (Insulin aspart)
Apidra ® (Insulin glulsine)
Intermediate acting insulin
Humulin ® N or Novolin ® N (N=neutral protamine zinc hagedorn)
Mixture of intermediate acting /regular insulin
Humulin ® 70/30 or Novolin ®70/30
Novolog ® 70/30
Long acting insulin
Lantus ® (insulin glargine)
Levemir® (insulin detemir)
In general, insulin is the first line of therapy in type I DM.
In type II DM, oral drugs are tried first, ultimately insulin is
required in this class of people as well
10
Insulin Products
http://pixgood.com/novolog-logo.html
http://www.lantus.com/considering/lantus-solostar-features/lantussolostar-pen
http://www.diabeteshealth.com/
11
Insulin Products
12
Most insulin products are U100 insulin meaning 100
units/ml
Question: if the patient is to get 70 units of insulin at
bedtime. What is their dose in ml?
Answer: C*V=D
(100 units/ml) V (ml)= 70 units
V=70/100 or 0.70 ml
Insulin syringes are widely available where ml are
calibrated in units
13
Most insulin products are U100 except for a product
called Toujeo® which is insulin glargine (Lantus®) but
it is U300 insulin (300 units/ml)
14
New to the Market
Afrezza ®
Made by Mannkind Corporation
Released January 2016
Inhaled human insulin, not injected
Similar to short acting insulin product
Contraindicated in patients with COPD and Asthma
15
Oral Drugs for Diabetes Mellitus
Type I DM patients can not be treated with most of these
drugs
Used in Type II DM
Sulfonyureas
Increases insulin secretion from the pancreas
Should be given with food
Avoid Alcohol
Glipizide (Glucotrol®)
Glyburide (Diabeta®)
Tolbutamide (Orinase®)
Glimepiride (Amaryl®)
Biguanides
Inhibits hepatic gluconeogenesis during fasting
Metformin (Glucophage®)
Caution: with people with kidney disease can result in a fatal
reaction called Lactic acidosis
16
Meglitinides
Similar to sulfonylureas
Taken before a meal
Repaglinide (Prandin®)
Nateglinide (Starlix®)
Thiazolidinediones
Also known as the glitazones
Increases insulin sensitivity in adipose tissue and
muscles
Pioglitazone (Actos®)
Rosiglitazone (Avandia®)
17
Novel New Drugs
dipeptidyl peptidase- 4 inhibitors
Blocks an enzyme in the kidney called dipeptidyl
peptidase- 4
Blockade of this enzyme allows a hormone called
glucagon like peptide I or GLP1 to last longer
GLP1 helps augment insulin release in response to a
sugar rich meal
Onglyza ®(saxagliptin)
Januvia ® (sitagliptin)
Tradjenta® (linagliptin)
Incretin Mimetics (GLP like)
Exenatide (Byetta®)
Liraglutide (Victoza®)
Injectable hormones
GLP-1 agonists
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Gliflozin Drug
MOA: blocks a key sodium channel in the kidney called
SGLT2. Glucose “piggybacks” with sodium as sodium is
reabsorbed by the kidneys. This lowers blood glucose
and glucose in eliminated in the urine with sodium
Side effects
Hypoglycemia
Low blood pressure
Urinary tract infections
Candiasis in women
Examples
Generic Name
Brand Name
Canaglifozin
Invokana ®
Dapaglifozin
Farxiga ®
Empaglifozin
Jardiance ®
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Combination Tablets
Combination tablets are popular in the treatment of
diabetes and other medical conditions
Drug manufacturers combine two drugs with different
MOA
Reduces amount of tablets patients take
Disadvantage: can’t alter the dose of one component
without altering the dose of the other
Drug Product
Components
Metaglip ®
Metformin / Glipizide
Actoplus Met
Pioglitazone/ Metformin
Glucovance
Metformin/ Glyburide
Duetact
Glimepiride/ Pioglitazone
20
Thyroid Disease
Thyroid gland is responsible for secreting thyroid
hormone, T4.
T4 basically controls metabolic functions in the body
More T4 equals a higher basal metabolic rate
Less T4 equals a lower basal metabolic rate
Hypothyroidism is a condition where thyroid gland does
not secrete adequate T4
Condition products slow BMR, slow heart rate, electrolyte
abnormalities, lipid disorders
Tx: Levothyroxine (synthroid ®, Levoxyl ®)
Hyperthyroidism is a condition of to much T4
Can produce a dangerous heart condition called Atrial
Fibrillation
Tx: Methimazole (Tapazole®), Propylthiouracil (PTU)
SSKI (super saturated potassium iodide) used in the
emergency tx of “thyroid storm”
21
Corticosteroids
Adrenal gland naturally produces cortisol and other “corticosteroids”
These hormones are very important in priming the body to deal with
stress.
A loss of cortisol secretion by the adrenal gland produces “adrenal
crisis” which is a medical emergency
Drugs should not be stopped abruptly; must be “tapered”
Generic
Brand
Prednisone
Deltasone®
Methylprednisolone
Medrol ®(oral)
Solu Medrol ®(IV)
Dexamethasone
Decadron®
Hydrocortisone
Hytone® (topical)
Solucortef ®(IV)
Severe side effects: immune suppression, osteoporosis,
elevated blood glucose, cataracts, growth suppression in
children
With Inhalation products like Advair® tell patients to rinse
mouth after the dose
22
The Nervous System
Divided into central nervous system (CNS) and
peripheral nervous system (PNS)
Central nervous system
Includes brain and spinal cord
Controls all nervous system functions
Control may be direct or indirect
Peripheral nervous system
Includes all other nerves and sensory organs
Controlled by central nervous system
Divided into somatic and autonomic nervous systems
23
Functions of the Nervous System
Sensory (afferent)
Sends impulses from other parts of body toward the
CNS
Senses external changes or conditions in the
environment, such as cold or heat
Senses internal changes in the body, such as decrease in
potassium or calcium
Integrative
Processes perceived information about the sensory
changes
Interprets or explains changes in external/internal
environments
24
Neuron
Smallest unit of the
nervous system
Brain is composed of
approximately 100
billion neurons
Highly differentiated
from other cells
25
Neurotransmitters
Released at the end of the neuron
Synapse is the space between two different
neurons
Neurons transfer information by crossing
synapses
Neurotransmitters travel across the synapse to
reach a receiving neuron
Attach to special structures called receptors
Communicate with and control glands, organs,
and muscles
26
Central Nervous System Drugs
Sedatives and Tranquiller: Drugs that cause depression of
the reticular activating system in the brain. Differences in
mechanisms of action.
Examples are
barbiturates: Phenobarbital (Luminal®)
Benziodiazepines: Chlordiazepoxide (Librium®), Diazepam
(Valium®), Lorazepam (Ativan®), Alprazolam (Xanax®)
BDZ were developed in the 1960’s with the advent of librium®.
BDZ are safer than barbiturates. Both dangerous with alcohol
consumption.
Used in anxiety disorder, panic disorder, GAD, sleep disorders
Control Substance: CIV
Miscellanous agents in the class are zolpidem (Ambien®),
zaleplon (Sonata®)
CNS Depressants
Benzodiazepines and Barbiturates
MOA: binds to GABA receptors in brain
Indications: sedation for anxiety and pre op use
Main Side Effect: drowiness, Dependence (CIV)
Secobarbital prescribed for physician assisted suicide
Generic
Brand
Lorazepam
Ativan
Clonazepam
Klonopin
Alprazolam
Xanax
Midazolam
Versed
Phenobarbital
Luminal
Secobarbital
Seconal
Depression
Symptoms include feelings of despair, lack of energy,
inability to concentrate
Related to decreases in concentration of the
neurotransmitters
Treated with drugs that:
Block the reuptake of neurotransmitters
TCA (tricyclic antidepressents)
Nortripyline (Pamelor®), Amitripyline (Elavil®)
Dangerous in overdose
Doses over 500 mg can be fatal
SSRI
Fluoxetine (Prozac®)
Paroxetine (Paxil®)
Sertraline (Zoloft®)
Citalopram (Lexapro)
SNRI
Duloxetine (Cymbalta®) (used to treat neuropathic pain also)
Safer in overdose than TCA’s
29
Interfere with the breakdown of the monoamines within
the synaptic cleft
MAOI
Used in the 50 and 60’s
Very dangerous in overdose
Many drug interactions especially with hypoglycemic drugs
and antihypertensive drugs
Drug food interactions with foods with high tyramine content
like cheeses, wine, chocolates, etc
Phenelzine (Nardil®)
Tranylcypromine (Parnate®)
Used now only a last ditch effort to treat SSRI resistant
depression
If a patient is switch to a different antidepressant must
wait 14 days after stopping MAOI before starting new
drug, called “wash out period”
30
Psychosis
State in which a person is out of touch with reality
One cause may be an increase in dopamine
Treated with antipsychotic drugs that attach to the dopamine D2
receptor
Treated with dopamine receptor antagonists
Generic
Brand
Haloperidol
Haldol ®
Chlorpromazine
Thorazine®
Fluphenazine
Prolixin®
Thioridazine
Mellaril ®
Major side effects: Abnormal heart arrhthymias,
hypotension, sedation, Extrapyramidal symptoms
(Parkinson’s like) movement disorders
31
Second Generation Antipsychotics
The previous list of Antipsychotics had major side effects of
hypotension, sedation, weight gain, erectile dysfunction, cardiac
arrhythmias (Long QT) and EPS (Extra pyramidal Symptoms)
EPS is a movement disorder that is similar to Parkinson’s disease
Second generation drugs were developed to avoid EPS
A major side effects to these drugs are: risk of drug induced diabetes
and weight gain.
Clozapine has the risk of fatal blood condition called agranulocytosis
(Very low white blood cell count)
FDA REMS requires registries set up to monitor this risk
Generic
Brand
Olanzapine
Zyprexa
Clozapine
Clozaril
Quetiapine
Seroquel
Risperidone
Risperdal
Ziprasidone
Geodon
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Parkinson’s Disease
basal ganglia of the brain effected
These neurons are dopaminergic and secrete
dopamine as a neurotransmitter
These neurons coordinate with neurons in the motor
cortex to help initiate movement
Signs and symptoms
Resting tremor: shaking limbs and hands at rest which goes
away with movement (first sign noticed by family or patient)
Gait imbalances: patient has problems initiating movement
and may show signs of bradykinesia and muscle rigidity often
called dystonia
33
Treatment of PD
Dopaminergic drugs
Used to “replace” dopamine in the brain
Taken orally
Sinemet® Carbidopa/Levodopa
Levodopa is converted to dopamine in the brain
Dramatically improves symptoms
Often effective for several years before drug resistance sets in
Dopaminergic type drugs
Ergot alkaloid drugs that act at dopamine receptor
Bromocriptine (Parlodel)
Cabergoline (Dostinex®)
Ropinirole (Requip®)
34
Antiepileptics
Indications: Drugs used to treat seizures. Off label
use: Neuropathic pain
MOA: Many of the drugs block the sodium ion
channel in nerves and stop the neuron from
“firing”
Main Side effects: Drugs in this group are known
to cause birth defects
Levetiracetam is a known cause of SJS
Topiramate can cause kidney stones
For emergency tx of status epilepticus : use diazepam or
phenytoin IV
Generic
Brand
Phenytoin
Dilantin
Valproic Acid
Divalproex Sodium
Depakene
Depakote
Carbamazepine
Tegretol
Gabapentin
Neurotin
Oxcarbazepine
Trileptal
Levetiracetam
Keppra
Topiramate
Topamax
Phenytoin, Valproic acid, Levetiracetam and Diazepam are available as
IV injections
Drugs used to treat Alzheimer
Disease
Alzheimer disease is a degenerative neurological
disease of primarily cholinergic neurons
Results in loss of memory, personality changes and
complete loss of language skills
Generic
Brand
Donepezil
Aricept
Memantine
Namenda
Rivastigmine
Exelon
Drugs used to treat ADHD in children and adults
Mixed amphetamine salts: Adderall® XR
Other agents: Methylphenidate (Ritalin® Concerta ®,
Focalin ®)
Atomoxetine (Strattera ®)
Lisadexamfetamine (Vyvanse ®)
Dextroamphetamine (Dexedrine ®)
All the above drugs are controlled substances except
Atomoxetine
The Immune System
Consists of two types
Humoral Immunity
Cell mediated Immunity
Humoral Immunity
Involves blood proteins
Is recruited when physical barriers like the skin are breached
Complement proteins are proteins in the blood that recognize
bacterial cells and other microorganisms.
They basically open holes in those cells and allow osmosis of water to
lyze and kill them
Antibodies
These are proteins that are secreted by an activated B lymphocyte
called a plasma cell.
Antibodies are highly specific for the bacteria, fungi, protozoa that
they target
39
Antibiotic mechanism of action
Penicillin and Cephalosporins: drugs inhibit the
formation of the bacterial cell wall. Bacteria swell and
die. Drugs are bactericidal
Macrolides: inhibits bacterial ribosomes and protein
synthesis. Example includes erythromycin (E-Mycin®)
and azithromycin (Zithromax®). Bactericidal or
Bacteriostatic.
Tetracyclines: Bacteriostatic by inhibiting protein
synthesis.
Fluroquinolones: Bactericidal. Binds to DNA gyrase
Aminoglycosides: (Gentamicin) Bactericidal by several
mechanisms
Penicillins and Cephalosporins are classified as Beta Lactam
antibiotics.
Very important antibiotics
Treats a wide variety of bacterial infections
Penicillins are several classes
Class
Example
Brand name
Natural Penicillin Penicillin G
Pfizerpen (IV
form)
Veetids (tablets)
Aminopenicillin
Ampicillin
Omnipen
Ureidopenicillin
Piperacillin/Tazo
bactam
Zosyn
Penicillinase
resistance
penicillins
Nafcillin
Nafcil
Aminopenicillin Amoxicillin +
+ Beta Lactamase Clavulanate
Inhibitor
Potassium
Augmentin
Main Side Effects of penicllins/cephalosporins
Nausea/Vomiting
Diarrhea
Type I hypersensivity
Cephalosporins
Chemically similar to penicillins (Beta lactam)
Four generations
Excellent antibiotics
Similar side effects
Generation
Generic
Brand
First
Cephalexin
Keflex (oral only)
Cefazolin
Ancef (IV)
Cefaclor
Ceclor (oral only)
Cefuroxime
Ceftin (oral
suspension)
Zinacef (IV)
Ceftriaxone
Rocephin (IV only)
Cefdinir
Omnicef (oral
only)
Fourth
Cefipime
Maxipime (IV only)
Carbapenems
Meropenem
Imipenemcilastatin
Merrem (IV only)
Primaxin (IV only)
Second
Third
Third and fourth generations are used to treat meningitis and
hospital acquired infections and pneumonias
Fluoroquinolones
Must take oral forms of these drugs separate from antacids (Maalox) by
1-2 hours
Many drug interactions
Advised to limit the consumption of caffeine while on these drugs
(ciprofloxacin more than others)
Used for URIs and UTI and GI tract infections
Fluoroquinolones are contraindicated in pregnant patients and patient
younger than 18 years old
Cipro ® comes in IV, oral tablets, opthalmic and oral suspension
Generic
Brand
Ciprofloxacin
Cipro
Levofloxacin
Levaquin
Moxifloxacin
Avelox
Lomefloxacin
Maxaquin
Tetracyclines
Broad spectrum antibiotic class
Effective for use in certain infections
Chlamydia and gonorrheal infections
Lyme Disease
Rocky Mountain Spotted Fever
Contraindicated in pregnant women and young children < 8 years old
CAUTION: never use expired tetracycline products. Toxin produces serious
kidney damage
CAUTION: advise patient to wear protective clothing. Drugs are
photosensitive chemicals
Generic
Brand
Doxycycline hyclate
Vibramycin
Doxycycline
Monohydrate
Monodox
Minocycline
Minocin
Macrolides and Ketolides
Commonly used to treat UTI like walking pneumonia and chronic
bronchitis
Notorious for GI side effects
Contraindicated in patient with hepatic dysfunction and QTc
prolongation (a EKG cardiac abnormality that can lead to VF and
death)
Patient should take macrolides with food
CYP450 inhibitors- many drug interactions
Generic
Brand
Azithromycin
Zithromax
Clarithromycin
Biaxin
Erythromycin base
E-Mycin
Erythromycin
ethylsuccinate
EES
Telithromycin
Ketek
Aminoglycosides
Used to treat severe life threatening infections
IV formulations of AG are toxic to the kidney and to
cranial nerve VIII causing hearing loss (ototoxicity)
Requires monitoring of renal function and blood levels
of these drugs
Generic
Brand
Gentamicin
Garamycin
Amikacin
Amakin
Tobramycin
Nebcin
Miscellaneous Antibiotics
Generic
Brand
Indication(s)
Adverse
Reactions
Vancomycin
Vancocin
Meningitis,
Pneumonia,
MRSA
Renal toxicity
Clindamycin
Cleocin
URI, Acne, female Increased risk of
genital infections, C. Difficile Colitis
dental
prophylaxis for
pen allergic
patients
Metronidazole
Flagyl
GI tract
infections and
protozoal
infections
Severe reaction
when taken with
alcohol
Linezolid
Zyvox
Meningitis,
Pneumonia,
MRSA
Reaction with
MAOI
antidepressants
Viral Infections
Virus are non living things who primary reason for
existence is to make more copies of themselves
Infect various cells. Each virus may have its own
preference called a virus’ trophism
Antibiotics can not be used to treat these infections
Antiviral Drugs
Acyclovir
Gancyclovir
Ribavirin
These drugs usually acted on a viral DNA or RNA
polymerase blocking its action
49
Antiviral Drugs
Most viral infections are self limiting
Severe case of herpes, cytomegalovirus, and Influenza
are amenable to drug therapy
Generic
Brand
Virus
Acyclovir
Zovirax
Herpes
Valacyclovir
Valtrex
Herpes
Valganciclovir
Valcyte
CMV, Herpes
Famciclovir
Famvir
Herpes
Ganciclovir
Cytovene
CMV
Penciclovir
Denavir
Cream for oral
herpes
Oseltamavir
Tamiflu
Influenza
Zanamivir
Relenza
Influenza
(Inhalation
product)
50
Antihelminthics
Helminths are eukaryotic parasitic worms
Types
Cestode: Tapeworms
Trematode: Flukes (Flatworms)
Nematodes: Roundwords
All produces eggs and Larvae and have a complex life
cycle
Worms can exist in their human host for years and can
locate in different tissues
Intestine houses tapeworm
Blood houses schistosoma trematodes. Acute disease is called
Katayama’s Fever as worms are in the blood
Lungs houses paragonimus westermani. Pulmonary
Paragonimiasis appears as a severe pneumonia
51
Antihelminthics
Brand
Generic
Major Indication
Albenza
Albendazole
Pinworms, tapeworms
Stromectol
Ivermectin
Many types of worms
including larval
heartworm in dogs. Used
for lice, scabies and
bedbugs
Biltricide
Praziquantel
Many type of worms
Ergamisol
Levamisole
Dewormer used in
veterinarian medicine for
livestock. Nicotinic
receptor agonist
52
HIV infection
Target of HIV is the CD4 lymphocyte
HIV also shows trophism to the macrophage and a cell
in the CNS called a microglial cell
RNA virus that replicates inside of CD4 cell
CD4 cells die as virus is released and starts a new
round of infection.
Infection can not be cured; the virus spread to
macrophages which can live for years provides a life
long viral reservoir.
53
Natural History of HIV infection
Exposure to blood or bodily fluids through sexual
contact and/or use of needles
Prodromal stage
Initial stage of infection: about 4 weeks patient develops
signs of flu like symptoms
Before this period no antibodies against HIV can be
deteched
After this febrile flu like state passes, patient is said to be
seroconverted (i.e. will show detectable antibodies)
Clinical latency
The immune system temporarily subdue infection
Can last between 2-10 years
As virus replicates in CD4 cells, these cells die by
rupture, apoptosis or attack by the CD8 cell
As CD4 levels decline, opportunistic infection sets in
54
Acquired Immunodeficiency
Syndrome
Final Stage
Occurs when CD4 levels have fallen to less than 200
cells/microliter
And patient has one of the following
Pneumocystic Pneumonia caused by a protozoan,
Pneumocytis Jirovecci
Esophageal candidiasis
MAC infection
Kaposi Sarcoma
Burkitt’s Lymphoma
Patient will usually die from one of these cancers or
infections
55
Drugs used in HIV infections
Reverse transcriptase inhibitors
Block RNA reverse transriptase (NRTI)
AZT, Zidovudine (Retrovir®)
Abacavir (Ziagen®) known as ABC
Lamivudine (Epivir®) known as 3TC Approved for both HIV
and HBV
Emtricitabine (Emtriva®) also called FTC
Tenofovir (Viread®) approved for both HIV and HBV
Known as TDF
Didanosine (Videx ®) known as DDI
These drugs also come in various combinations
Combivir (AZT and Lamivudine) known as CBV
Emtricitabine-tenofovir (Truvada®)
NNRTI
Efavirenz (Sustiva®) also known as EFZ
Etravirine (Intelence®)
Rilpivirine (Endurant®)
56
Protease Inhibitors
Kaletra ® (lopinavir/Retrovir)
Reyataz ®(atazanavir)
Aptivus® (Tipranavir)
Prezista ® (Darunavir)
Lexiva ® (fosamprenavir)
Viracept ® (nelfinavir)
Norvir ® (Ritonovir)
Inhibits viral enzyme HIV protease which assists in viral
assembly
Norvir and Aptivus are stored in the refrigerator
57
Integrase Inhibitors
Integrase is an enzyme HIV uses to assembly viral
proteins
Drugs that block this enzyme
Dolutegravir (Tivicay®)
Elvitegravir (Vitekta®)
Raltegravir (Isentress®)
58
Booster medication
Cobicistat (Tybost®)
Drug is a strong inhibitor of CYP 450 liver enzymes
Blocks metabolism of other HIV medications
Used in combination drug products
Elvitegravir/Emtricitabine/Tenofovir + cobicistat
Brand name is Stribild ®
Many drug interactions
A great list of HIV medication names can be found at:
https://aidsinfo.nih.gov/education-materials/fact-
sheets/21/58/fda-approved-hiv-medicines
59
Fusion Inhibitors
Prevent HIV from attaching to CD4 cells
Pharmacology is very complex
Prevents “fusion” of virus with the cell
Drugs include:
Enfurvirtide (Fuzeon®) a drug given by subcutaneous
injection
Maraviroc (Selzentry®) oral drug
60