pharm notes - neil medical group...page 3 volume 21, issue 2 group d: a laba/lama combination...

8
Headache disorders are very common in the elderly. As we age, causes of headaches shift from benign to more serious conditions and they can often present in an atypical manner. We are all fairly familiar with tension headaches and mi- graines, but did you know that these are only one category in the greater scheme of all headache disorders? Tension, mi- graine, hypnic, and cluster headaches are what are known as primary headache disorders, whereas second- ary headache disorders are a less commonly known sub- type that are more common in the elderly population (and often only occur in this population). Secondary headache disorders include giant cell arteritis/temporal arteritis, intracranial mass/ brain tumor, subdural hema- toma, cardiac cephalgia, ischemic stroke/transient ischemic attack, and medication overuse headache. Interest- ingly, primary headache disorders de- crease with age while secondary head- ache disorders become more prevalent. Also, causes of headaches shift from benign to more serious conditions. While tension headaches are the most prevalent type of headache in the elder- ly and consist of peri-cranial tenderness and band tightening around the head, secondary headaches do pose a rather large problem in the elderly as they are often inadequately diagnosed due to their specificity. Migraines are caused by peptide release (including calcitonin, substance p, and neurokinin A) along with the depletion of serotonin. These together cause vasodilation and headaches. This is why the drug class triptans came about since they increase 5ht (a pre- cursor of serotonin) as well as decrease vasodilation. Mi- graines consist of a prodrome, aura, headache, and post- drome. Migraine without aura (classical migraine) must in- clude > 5 attacks (not caused by another condition) that last 4-72 hours and include nausea/vomiting and/or pho- tophobia/phonophobia. They must also be unilateral, pulsating, aggravated by physical activity, and moder- ate/severe in pain. Migraine with aura must include > 2 attacks with > 3 features in- cluding > 1 fully reversible aura symptom, > 1 aura symptom developing gradu- ally over 4 minutes or 2 symptoms in succession, aura symptoms that do not last more than 60 minutes, and a migraine headache that follows aura within 60 minutes (also not caused by another disorder). Migraines can be caused by over use of analgesics, nifedi- pine/nitrates/hydralazine (all of these medications cause vas- odilation), alcohol, caffeine, processed meats, chocolate, aged cheese, MSG, aspartame, weather, smoke, noise, flash- ing lights, too much sleep, too little sleep, stress, hormonal change, and missing meals. Migraines can be treated with NSAIDS, ergots (although they are less favored as they cause hypotension), and triptans. Do keep in mind that trip- tans are contraindicated if there is a history of ischemic heart disease/coronary artery vasospasm, history of stroke or tran- sient ischemic attack, ischemic bowel disease, uncontrolled hypertension, hemiplegic or basilar migraine, or recent use of another triptan or of an ergotamine-containing medication. Headaches in the Older Adult A Publication of Neil Medical Group, The Leading Pharmacy Provider in the Southeast March/April 2018 PHARM NOTES Inside this issue: Headaches in the Older Adult 1 Update: COPD 2017 Gold Guide- lines 2-3 Headaches in the Older Adult: conclusion 4-5 Non-Traditional Drugs of Abuse: What the Clini- cian Should Know 6-7 Neil Medical Group Contact Information 8 Volume 21, Issue 2 Continued on page 4

Upload: others

Post on 01-Sep-2020

5 views

Category:

Documents


0 download

TRANSCRIPT

Page 1: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Headache disorders are very common in the elderly. As we

age, causes of headaches shift from benign to more serious

conditions and they can often present in an atypical manner.

We are all fairly familiar with tension headaches and mi-

graines, but did you know that these are only one category in

the greater scheme of all headache disorders? Tension, mi-

graine, hypnic, and cluster

headaches are what are

known as primary headache

disorders, whereas second-

ary headache disorders are a

less commonly known sub-

type that are more common

in the elderly population

(and often only occur in this

population). Secondary

headache disorders include

giant cell arteritis/temporal

arteritis, intracranial mass/

brain tumor, subdural hema-

toma, cardiac cephalgia,

ischemic stroke/transient

ischemic attack, and medication overuse headache. Interest-

ingly, primary headache disorders de-

crease with age while secondary head-

ache disorders become more prevalent.

Also, causes of headaches shift from

benign to more serious conditions.

While tension headaches are the most

prevalent type of headache in the elder-

ly and consist of peri-cranial tenderness

and band tightening around the head,

secondary headaches do pose a rather

large problem in the elderly as they are

often inadequately diagnosed due to

their specificity.

Migraines are caused by peptide release

(including calcitonin, substance p, and

neurokinin A) along with the depletion of serotonin. These

together cause vasodilation and headaches. This is why the

drug class triptans came about since they increase 5ht (a pre-

cursor of serotonin) as well as decrease vasodilation. Mi-

graines consist of a prodrome, aura, headache, and post-

drome. Migraine without aura (classical migraine) must in-

clude > 5 attacks (not caused

by another condition) that

last 4-72 hours and include

nausea/vomiting and/or pho-

tophobia/phonophobia.

They must also be unilateral,

pulsating, aggravated by

physical activity, and moder-

ate/severe in pain. Migraine

with aura must include > 2

attacks with > 3 features in-

cluding > 1 fully reversible

aura symptom, > 1 aura

symptom developing gradu-

ally over 4 minutes or 2

symptoms in succession,

aura symptoms that do not last more than 60 minutes, and a

migraine headache that follows aura within 60 minutes (also

not caused by another disorder).

Migraines can be caused by over use of analgesics, nifedi-

pine/nitrates/hydralazine (all of these medications cause vas-

odilation), alcohol, caffeine, processed meats, chocolate,

aged cheese, MSG, aspartame, weather, smoke, noise, flash-

ing lights, too much sleep, too little sleep, stress, hormonal

change, and missing meals. Migraines can be treated with

NSAIDS, ergots (although they are less favored as they

cause hypotension), and triptans. Do keep in mind that trip-

tans are contraindicated if there is a history of ischemic heart

disease/coronary artery vasospasm, history of stroke or tran-

sient ischemic attack, ischemic bowel disease, uncontrolled

hypertension, hemiplegic or basilar migraine, or recent use of

another triptan or of an ergotamine-containing medication.

Headaches in the Older Adult

A Publication of Neil Medical Group, The Leading Pharmacy Provider in the Southeast

March/April 2018

PHARM NOTES

Inside this issue:

Headaches in the

Older Adult

1

Update: COPD

2017 Gold Guide-

lines

2-3

Headaches in the

Older Adult:

conclusion

4-5

Non-Traditional

Drugs of Abuse:

What the Clini-

cian Should

Know

6-7

Neil Medical

Group Contact

Information

8

Volume 21, Issue 2

Continued on page 4

Page 2: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Update: COPD 2017 GOLD Guidelines

Page 2

PHARM NOTES

Chronic obstructive pulmonary disease (COPD) is a chronic

disorder of the airways and the third leading cause of death in

the United Sates. COPD represents the second leading cause of

disability and is responsible for nearly 50 million physician

visits in the past 20 years. The economic impact is substantial

and cost about $32 billion in 2010. By 2020, the financial bur-

den is expected to reach $49 billion.

Chronic inhalation of harmful agents including tobacco smoke

and occupational pollution causes an abnormal inflammation

of lung airways and results in progressive airflow limitations.

Several structural changes occur such as narrowing of small

airways and destruction of lung parenchyma. COPD differs

from asthma in that airflow limitations are not fully reversible.

Risk factors for COPD include tobacco smoking, occupational

exposure, genetics, and environmental pollution. Hallmark

symptoms of COPD include dyspnea (shortness of breath),

chronic cough, and chronic sputum production. It is recom-

mended a patient with key symptoms and risk factors undergo

a spirometry test in order to definitively diagnose COPD. A

spirometry test measures the volume of air forcibly exhaled in

one second (forced expiratory volume - FEV1) compared to the

volume of air forcibly exhaled after taking the deepest possible

breath (forced vital capacity, FVC). This is referred to as the

FEV1/FVC ratio. Patient FEV1/FVC results are compared to a

reference range derived from healthy patients of the same age,

sex, and height. A value of FEV1/FVC < 0.7 confirms a diag-

nosis of COPD.

The Global Initiative for Chronic Obstructive Lung Disease

(GOLD) devised treatment guidelines with evidence-based

recommendations. These guidelines were recently revised in

2017. Per the guidelines, patients must be classified by both

airflow limitation severity and symptom burden/exacerbation

risk in order to determine the most appropriate COPD manage-

ment. In patients with an FEV1/FVC < 0.7, airflow limitation

severity is classified into groups GOLD 1-

4 based on their FEV1 percent predicted

(Table 1). Assessment of symptoms/

exacerbation risk are scored from A-D.

Guideline updates indicate that therapy

should be selected based off letter score

(A-D) and no longer GOLD 1-4 severity

classification (see Table 2). Both CAT

and mMRC scores are acquired through

patient questionnaires regarding how

symptoms, such as dyspnea, affect their

quality of life.

Past GOLD guidelines only recommended

initial therapy, however, the 2017 GOLD

revision suggests escalation and de-

escalation options for patients that are

already on treatment. Pharmacologic rec-

ommendations for stable COPD per the

GOLD 2017 guidelines are as follows:

Group A: A bronchodilator

Bronchodilators increase FEV1 by altering airway

smooth muscle tone, opening airways

A few examples include albuterol (short-acting

beta-2-agonist: SABA), salmeterol (long-acting

beta-2 agonist: LABA), ipratropium (short-acting

anticholinergic: SAMA), and tiotropium (long-

acting anticholinergic: LAMA)

Group B: A long-acting inhaled bronchodilator (either

a LABA or LAMA) Patients with persistent symptoms should add on a

second long-acting inhaled bronchodilator from

the other class

Group C: A long-acting inhaled bronchodilator - spe-

cifically a LAMA

Patients with persistent symptoms may benefit

from a second long acting bronchodilator (LAMA/

LABA combo) or switching to a combination of a

long-acting beta-2-agonist and an inhaled cortico-

steroid (LABA/ICS). Note: Adding an ICS in-

creases patient risk of developing pneumonia.

Page 3: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Page 3

Volume 21, Issue 2

Group D: A LABA/LAMA combination

LABA/ICS might be first choice for certain patients with co-existing asthma or a high eosinophil count.

Patients with persistent symptoms on LABA/LAMA may escalate to LABA/LAMA/ICS or switch to LAMA/ICS.

Patients on LABA/LAMA/ICS with an FEV1 < 50% predicted and chronic bronchitis may add roflumilast,

a macrolide antibiotic (azithromycin), or stop the ICS if no significant results were found.

Roflumilast is a phosphodiesterase-4 (PDE4) inhibitor that works by reducing inflammation in the air-

ways.

In addition to management of COPD symptoms by pharmacologic

treatment, several non-pharmacologic interventions are also rec-

ommended. If applicable, smoking cessation is key to preventing

disease progression and nicotine replacement therapy or pharma-

cologic therapy is recommended due to increased long-term smok-

ing abstinence rates. Patients in Groups B-D are also encouraged

to receive pulmonary rehabilitation. All patients, regardless of

classifications, should receive the pneumococcal vaccination as

well as the yearly influenza vaccination. Additionally, the new

guideline revisions added regular inhaler technique assessment in

order to improve therapy outcomes.

Despite effective medications, COPD exacerbations still occur

with the most common culprit being respiratory tract infections.

Fortunately, more than 80% of exacerbations can be treated in an outpatient setting. An exacerbation is defined as an acute

worsening of respiratory symptoms that requires additional therapy. COPD exacerbations are classified into three stages based

on severity. Mild exacerbations are treated in the out-patient setting and only require an addition of a SABA (e.g. albuterol). A

moderate exacerbation is treated with a SABA plus antibiotics and/or oral corticosteroids.. The recommended corticosteroid

dosing is 40 mg of prednisone once daily for 5 days. The recommended duration of antibiotic therapy is 5-7 days and antibiotic

choice should be based on local resistance patterns and patient risk factors for P. aeruginosa. Severe exacerbations require hos-

pitalization and recommends all components of moderate treatment as well as respiratory support. Options for respiratory sup-

port include oxygen therapy, ventilatory support, and non-invasive or invasive mechanical ventilation based on symptom se-

verity, PaO2, and O2 saturation.

Table 2: Assessment of Symptoms/Risk of Exacerbation

Table 1. Classification of airflow limitation severity in COPD (Based on post-bronchodilator FEV1 )

In patients with FEV1/FVC

GOLD 1: Mild FEV1 > 80% predicted

GOLD 2: Moderate 50% < FEV1 < 80% predicted

GOLD 3: Severe 30% < FEV1 < 50% predicted

GOLD 4: Very Severe FEV1 < 30% predicted

Article by Jessica Haynes, PharmD Candidate

Wingate University School of Pharmacy

Exacerbation History

> 2 or > 1 leading to

hospital admission

C

D

0 or 1 (not leading to

hospital admission)

A

B

mMRC 0-1 CAT < 10

mMRC > 2 CAT > 10

Page 4: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Page 4

Headaches in the Older Adult………………….continued from page 1

PHARM NOTES

Migraines can be prevented with valproic acid, beta blockers

(metoprolol/propranolol/timolol), topiramate, tricyclic antide-

pressants (try to avoid amitriptyline and imipramine as they

are more anticholinergic and instead go with nortriptyline or

desipramine), magnesium, venlafaxine, feverfew, and

NSAIDS. Do keep in mind that it takes 2-3 months for

prophylactic medica-

tions to work.

Tension headaches are

the most common

type of headache in

the elderly and they

present with peri-

cranial tenderness

with band tightening

around the head.

Neurobiological evi-

dence suggests epi-

sodic peripheral pain

mechanisms with

chronic central pain

mechanisms as the

cause. Episodic ten-

sion headaches must

include > 10 episodes

occurring over 3

months (not caused by

another disorder) that last 30 minutes to 7 days with no nausea

or vomiting and no more than 1 photophobia or phonophobia

event. They must also have at least > 2 features including

bilateral pain, pressing/tightening (non pulsating), mild to

moderate pain, and no aggravation by physical activity. Re-

member that a maximum of 2 grams of Tylenol per day is rec-

ommended in patients with liver disease while 3.25 grams of

Tylenol per day is recommended in regular patients to prevent

liver toxicity.

The one lesser known primary headache is what is called a

hypnic headache. Hypnic headaches are unique to the elderly

and you must be at least 50 years old in order to be diagnosed

with this headache subtype. They involve disturbance of

sleep-related physiology of the brain stem during REM sleep

partially due to a decrease in secretion of melatonin related to

the aging process. This in turn causes awakening a few hours

after sleep begins and lasts 15-180 minutes. First line therapy

is lithium carbonate. Indomethacin, caffeine, and melatonin

can be used as second line therapy if lithium is contra-

indicated. Criteria for hypnic headaches must include four of

the following criteria: it occurs only during sleep and awakens

the patient (and is not caused by another disorder); it has no

autonomic symptoms and no more than one symptom of nau-

sea, photophobia, or phonophobia; it lasts > 15 minutes after

awakening; and it has at least 2 of 3 characteristics including

it occurs > 15 times per month, lasts > 15 minutes after awak-

ening, and first occurs after the age of 50 years.

The first secondary

headache that is

seen in the older

adult is giant cell

arteritis. These are

due to chronic vas-

culitis and they

commonly affect the

cranial branches/

aortic arch including

the temporal and

ophthalmic arteries.

Giant cell arteritis is

commonly bi-

temporal and may

radiate via a throb-

bing pain to the

neck, jaws, face,

and tongue. It also

commonly causes

fever, anemia, fa-

tigue, anorexia, depression, generalized muscle aches, poly-

myalgia, rheumatic jaw claudication, diplopia, visual field

loss, amaurosis fugax, and blindness. It can be diagnosed

through lab work as it increases the ESR to > 50 mm/hour and

increases CRP. It can also be diagnosed via a temporal artery

biopsy. High doses of corticosteroids should be started imme-

diately upon suspected diagnosis of GCA and treatment must

continue for several months. Three of the five criteria must be

met in order to qualify giant cell arteritis including: age of

disease onset > 50 years old, new headache, temporal artery

abnormality (aka tenderness to palpate or decreased pulsa-

tion), erythrocyte sedimentation rate (ESR) > 50 mm/hour,

and abnormal temporal artery biopsy.

The next secondary headache category is medication overuse

headaches. They are often caused by opioids (which do not

have much evidence in effectiveness when used to treat head-

aches). Opioids also decrease the effectiveness of other abor-

tive medications such as triptans, NSAIDS, and ergotamines.

Also, medications that relieve headaches can cause medica-

tion overuse headaches (including triptans, ergotamines,

NSAIDS, APAP, ASA, and products containing butalbital).

Page 5: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Page 5

Volume 21, Issue 2

Medication overuse headaches present with mild-moderate symptoms, are commonly bilateral in location, cause diffuse pressure

as well as scalp tenderness, may be provoked by slight physical or mental activity, and are worse upon awakening (as the previ-

ous dose of offending medication wears off). The headache either resolves or returns to baseline pattern within 2 months. The

best treatment includes discontinuing/tapering the offending agent. Prophylactic therapy should also be considered. If acute

treatment is needed, then hydroxyzine, baclofen, tizanidine, neuroleptics, benzodiazepines, metaxolone, or methocarbamol can

be used.

Brain tumors are the next class of secondary headache. Interestingly enough, the tumor itself does not cause the headache. It is

instead caused by pressure from the tumor or pressure from the tumor related to fluid buildup. These in turn affect pain sensi-

tive blood vessels/nerves in the brain. Brain tumors often originate from lung, breast, kidney, and gastrointestinal cancer as well

as melanomas. They most commonly manifest as astrocytomas, oligodendrogliomas, meningiomas, and pituitary adenomas.

Headaches caused by brain tumors are insidious and gradual/progressive in nature. The patient will have symptoms 20-50% of

the time and pain is usually occipital in location (back/base of head). However, certain types of tumors can cause more frontal

pain. Tension-type headaches are the most common type of headache associated with brain tumors. They are also worse in the

morning (upon waking/rising) and cause vomiting and increased intracranial pressure that is most often resistant to common

analgesics. Patients who already have a history of headaches will now have more severe and frequent headaches that are associ-

ated with seizures, mental status change, and hemiparesis. Treatment varies based on the symptoms, tumor type, functional sta-

tus, disease progression, and current medications already treating the tumor. If treatment is palliative, then pain should be man-

aged aggressively with analgesics, opioids, and glucocorticoids.

In closing, always treat any new onset headache in the older adults as a possible serious condition. It is always beneficial to

evaluate brain imaging, metabolic monitoring (high calcium, low thyroid), and inflammatory markers in order to evaluate the

possibility of secondary headache disorders. Also, always keep in mind that primary headaches often present atypically in the

elderly. Be sure to also rule out drug-induced causes. Lastly, always look for contraindications to comorbid medical conditions

as well as medications that limit negative consequences (such as drugs on the BEERS list) due to the general senescence of the

body as it ages.

TYPE OF HEADACHE ABORTIVE TREATMENT PROPHYLACTIC TREATMENT

MIGRAINE Mild-Moderate: NSAIDs or combination

APAP + ASA + Caffeine

Moderate-Severe: Triptans or ergots

1st Line: Valproic Acid, Metoprolol, Propranolol,

Timolol, Topiramate, petasites

2nd Line: Tricyclic antidepressants, Atenolol, Mag-

nesium, Venlafaxine, NSAIDS, and feverfew

TENSION Mild-Moderate: APAP 1000mg per attack,

NSAIDs, ASA

Moderate-Severe: ***Triptans and Ergots

have NO ROLE***

1st Line: Tricyclic Antidepressants (Nortriptyline)

2nd Line: Venlafaxine, Mirtazapine

HYPNIC Aspirin 1st Line: Lithium Carbonate (avoid w/thyroid dys-

function, weight gain, tremor)

2nd Line: Indomethacin, caffeine, melatonin

GIANT CELL

ARTERITIS

Prednisone 60-80mg daily

Treat until symptoms remit (normally treated for sev-

eral months) and ESR normalizes, then taper over 2-4

weeks

MEDICATION

OVERUSE

HEADACHE

1st Line: Discontinue/taper offending agent

2nd Line: Hydroxyzine, Baclofen, Tizanidine,

Neuroleptics, Benzodiazepines, Metaxolone,

Methocarbamol

Article by Rachel Benton, Pharm D, BCGP

Page 6: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Non-Traditional Drugs of Abuse Advice for the Clinician

Page 6

PHARM NOTES

Many medications that are prescribed and used routinely

have the potential for abuse. The most likely pharmaceuticals

include those that may have psychoactive effects such as in-

creased energy, intoxication, sedation, relaxation, hallucina-

tions and euphoria. Patients may seek out these medications

legally, obtain them from family or friends, or drug dealers.

If taken in large enough quantities, they may experience psy-

chogenic effects that may lead to abuse.

Common OTC medications that may be abused include

cough/cold preparations (containing antihistamines, decon-

gestants and dextromethorphan) and antiemetics (such as Cy-

clizine and Dimenhydrinate). Prescription medications which

are not “scheduled” indicating abuse potential, include anti-

cholinergics, H2 blockers, hypertensive medications, antide-

pressants, atypical antipsychotics, and anticonvulsants. Alt-

hough it is difficult to pinpoint exactly why these medica-

tions are abused, their effects may include euphoria, dissocia-

tive and hallucinogenic effects, or potentiation of psychogen-

ic effects when combined with other drugs. When these com-

mon drugs are abused, typically excessive dosages are used

and the routes of administration are changed.

This article will focus on some commonly used medications:

atypical antipsychotics, anticonvulsants, antidepressants, and

skeletal muscle relaxants.

ATYPICAL ANTIPSYCHOTICS

Quetiapine (Seroquel) is repor ted as the most abused an-

tipsychotic. When taken in large doses, sometimes intrana-

sally, it may have sedative and anxiolytic effects. Prison in-

mates have described it as “quell” or “baby heroin” and its

abuse has led to removal from several prison formularies.

“Quell” may be obtained from drug dealers indicating it has

“street value” just like the more commonly abused opioid

medications. It is often mixed with recreational drugs for

“getting mellow” or “slowing down”.

Olanzepine (Zyprexa) has similar effects and has been

used “for a buzz” or euphoria. Abusers may take excess oral

doses, inject dissolved tablets, or use in combination with

alcohol, opioids, cocaine/crack, methamphetamine, cannabis

and benzodiazepines. The combination may enhance the

effects of other drugs or counteract adverse effects of illicit

substances.

Other antipsychotics with abuse reports include risperidone,

aripiprazole, ziprasidone and asenapine. Recent studies for

abuse of atypical antipsychotics have focused on psychiatric

patients. Clinicians should consider the risk of prescribing

medications for reasons other than psychosis, such as sleep,

anxiety, and depression, given their potential for misuse in

this patient population. Also, if a patient who has no known

history of a psychotic disorder requests an antipsychotic, this

should be a red flag.

ANTICONVULSANTS

Gabapentin (Neurontin) has been recognized as another

medication with addictive properties. Pregabalin, a similar

medication, is known to be addictive and is now a Schedule

V drug. Gabapentin is not a controlled substance and is indi-

cated for the treatment of epilepsy and post herpetic neural-

gia. As a GABA agonist, it slows down the activity of nerve

cells in the brain. Off label uses include pain syndromes,

anxiety and mood disorders, restless leg syndrome and alco-

hol withdrawal. In Europe, there have been at least 20 cases

of addition to gabapentin. Abusers describe it as “zombie-

like”, calming, euphoric and it increases their sociability. Ab-

ruptly stopping gabapentin causes withdrawal symptoms in-

cluding seizures, diaphoresis, agitation, confusion, and ele-

vated vital signs. Some symptoms, including catatonia, have

been similar to withdrawal from alcohol or benzodiazepines.

"All things are poisons, for there is nothing without poisonous qualities. It is only the dose which makes a thing a

poison,”

Paracelsus quoted.

Page 7: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

Page 7

ANTIDEPRESSANTS

Amitriptyline (Elavil) in large doses may produce eupho-

ria, relaxation, giddiness, and contentment. Other similar tricy-

clic antidepressants have the most potential for abuse due to

their anticholinergic or dopaminergic effects. In combination

with opiates, there may be a prolonged psychogenic effect. It

has been documented that patients in drug treatment centers

seek out TCAs to produce euphoria and pleasant auditory/

visual hallucinations. In one methadone program, up to 25% of

patients were using amitriptyline for euphoric effects.

Bupropion (Wellbutrin), a norepinephrine-dopamine

reuptake inhibitor, may be abused by nasal insufflation produc-

ing effects similar to cocaine. Prison inmates report it is very

addictive and has a cocaine-like feel and taste. Since nasal in-

gestion bypasses the first-pass metabolism, the drug has rapid

and higher concentration in the body.

Other antidepressants with abuse potential include Fluoxetine

(Prozac), Venlafaxine (Effexor) and Tranylcypromine

(Parnate). These medications taken by the “handful” can

cause insomnia and amphetamine-like effects. Higher dosing

can lead to tolerance, dependence and withdrawal upon discon-

tinuation. Again, these medications may be combined with

illicit drugs. For example, Prozac and Zoloft have both report-

ed to prolong the effect of ecstasy.

SKELETAL MUSCLE RELAXANTS

Due to their sedative properties, skeletal muscle relaxants have

abuse potential. Sometimes they are used in combination with

other depressive substances.

Baclofen (Lioresal) is a GABA receptor agonist. It is struc-

turally similar to the “date rape drug” and has been used by

teenagers. One adolescent party with abuse of Baclofen result-

ed in 14 hospitalizations and 9 intubations. It may cause eu-

phoria, sedation and amnesia effects.

Cyclobenzaprine (Flexeril) is structurally similar to ami-

triptyline and it has similar sedative and anticholinergic ef-

fects. There was an 87% increase of cyclobenzaprine-related

ER visits over 7 years in 2011.

Other relaxants such as carisoprodol (Soma) and Tizanidine

(Zanaflex) may be abused as well. Car isoprodol is metabo-

lized to meprobamate, a known highly addictive schedule V

drug. Meprobamate (Equagesic /Equanil) has multiple uses as

muscle relaxant, anticonvulsant, anxiolytic and hypnotic.

These medications may cause sedation and impair driving abil-

ity.

OTHER MEDICATIONS USED IN COMBINATION

Clonidine (Catapres) is an alpha agonist approved for

treatment of hypertension. Through this mechanism of action,

it reduces sympathetic response causing sedation, impaired

consciousness and seizures. Opiate addicts frequently use it to

decrease opioid withdrawal symptoms or for its psychogenic or

euphoric effects. It helps them tolerate long time periods be-

tween opioid consumption. Clonidine may also be abused in

combination with other drugs, particularly diazepam.

Cimetidine (Tagamet) is an H-2 blocker and indicated for

multiple gastrointestinal related diagnoses and off-label for

urticaria. It inhibits a number of enzymes (CYP 1A2, 2C19,

2D6, and 3A4) which are responsible for metabolizing other

medications, thereby increasing the effects of those medica-

tions. Taking cimetidine prior to methadone or cocaine in-

creases or prolongs the drug addict’s response to those abused

drugs.

Loperamide (Imodium) is called the “poor man’s metha-

done” and addicts use it at very high doses (70-100mg/day) to

decrease opioid withdrawal symptoms like muscle pains, vom-

iting, diarrhea and nausea at high doses. Note that the normal

dose is up to 8mg (4 pills) daily. Loperamide works in the

same way that opioids work in the body at the opioid receptor

in the GI tract; however, high doses will cross the blood brain

barrier and produce euphoria. Cases of sudden death, due to its

cardiotoxicity, have been reported in addicts with postmortem

levels of 200 times or greater of loperamide in their bodies.

THE CLINICIAN’S RESPONSE

Finally, the clinician should be aware of the potential for non-

traditional medications that may be abused alone or in combi-

nation with other drugs. As the internet forums show, addicts

share details of “how to” abuse both legal and illegal drugs.

Any medication that has psychoactive effects may be abused if

taken in higher doses or by alternative routes of administration.

Safe and diligent prescribing and monitoring of these medica-

tions should include appropriate indications along with com-

plete patient history of known psychiatric or abusive drug his-

tory.

Volume 21, Issue 2

Article by Melodie Seagle, PharmD, BCGP

Page 8: PHARM NOTES - Neil Medical Group...Page 3 Volume 21, Issue 2 Group D: A LABA/LAMA combination LABA/ICS might be first choice for certain patients with co-existing asthma or a high

PHARM NOTES

Kinston Pharmacy

2545 Jetport Road

Kinston, NC 28504

Phone 800 735-9111

Louisville Pharmacy

13040 East Gate Parkway

Suite 105

Louisville, KY 40223

Phone 866-601-2982

Mooresville Pharmacy

947 N. Main Street

Mooresville, NC 28115

Phone 800 578-6506

To all the Pharm Notes Family,

I am continuing to share excerpts from “The Letter”…...which was given to my granddaughter on

her 1st birthday and will be saved until she turns 18.

“Ten Ways to Not Make Your Life Harder than it Has to Be”

3. Don’t Fast Forward to the Apocalypse

I have always struggled with forwarding everything to its worst possible outcome and being pleas-

antly surprised when the result is marginally better than utter disaster or terminal illness. My mind

unnecessarily wrestles with events and outcomes that aren’t even remotely likely. My sore throat is

cancer. A call from my boss may mean my job is on the line. Negativity only breeds more negativity.

It is a happiness riptide. It will carry you far from the shore and if you don’t swim away from it, it

will pull you under.

4. Don’t Have Unrealistic and/or Uncommunicated Expectations

Reality Check: Your family and friends cannot read your mind or anticipate your thoughts or whims.

Did your boyfriend forget the six and a half month anniversary of your first movie date? Did a fami-

ly member forget to call you at an appointed hour? Did your best friend fail to fawn over your new

outfit? Unmet expectations will be at the root of most of the

unhappiness in your life. If you will minimize your expecta-

tions….you will maximize your joy.

To be continued…...next time……..

Cathy Fuquay

Pharm Notes Editor

Pharm Notes is a bimonthly publication by Neil

Medical Group Pharmacy Services Division.

Articles from all health care disciplines pertinent

to long-term care are welcome. References for

articles in Pharm Notes are available upon request.

Your comments and suggestions are appreciated.

Contact: Cathy Fuquay ([email protected])

1-800-735-9111 Ext 23489

...a note from the Editor

Thank you for allowing Neil Medical Group to partner with

you in the care of your residents!