KCl(po potassium chloride) - treatment of hypokalemia and associated conditions, for digitalis poisoning, and as an electrolyte replenisher. Brand names include K-Dur®, Klor-Con®, Micro-K®, and Kaon Cl®.
atenolol - selective beta blocker
lisinopril - drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in treatment of hypertension, congestive heart failure, heart attacks and also in preventing renal and retinal complications of diabetes.
darvocet - an analgesic in the opioid category. It is used to treat mild to moderate pain and as an antitussive. It can be used to ease pain before, during and after an operation. It is often combined with acetaminophen in the preparation co-proxamol (Darvocet in the US and CAPADEX in AUS).
diazepam - drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, skeletal muscle relaxant and amnestic properties. This makes it a useful drug for treating anxiety, insomnia, seizures, alcohol withdrawal, and muscle spasms. It is also used before certain medical procedures (such as endoscopies) to reduce tension and anxiety, and in some surgical procedures to induce amnesia.
oxybutynin - anticholinergic med to treat urinary/bladder muscle spasm
paroxetine - selective serotonin reuptake inhibitor(SSRI) antidepressant
aspirin - analgesic, anti-inflammatory, NSAID
terazosin - selective alpha-1 antagonist for treating prostate enlargement(benign prostate hyperplasia)
fosamax(alendronate) - biphosphate drug for treating osteoporosis
donepezil - acetyl cholinesterase inhibitor for treatment of Alzheimer's to increase cortical acetylcholine
------------------------------------------------------------------------------
Furosemide (INN) or frusemide (former BAN) is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by sanofi-aventis under the brand name Lasix.
Like other loop diuretics, furosemide acts by inhibiting the Na-K-2Cl symporter in the thick ascending loop of Henle. It also has inhibitory activity on carbonic anhydrase.
Additionally, furosemide is a noncompetitive subtype-specific blocker of GABAA receptors (Korpi et al, 1995, Tia et al, 1996, Wafford et al, 1996). Furosemide has been reported to reversibly antagonize GABA-evoked currents of alpha6 beta2 gamma2 receptors at microM concentrations, but not alpha1 beta2 gamma2 receptors (Korpi et al, 1995; Wafford et al, 1996). During development, the alpha6 beta2 gamma2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide (Tia et al, 1995).
[edit] Clinical use in humans
Furosemide, as a loop diuretic, is principally used in the following indications (Aventis, 1998):
- Edema associated with heart failure, hepatic cirrhosis, renal impairment, nephrotic syndrome
- Hypertension
- Adjunct in cerebral/pulmonary edema where rapid diuresis is required (IV injection)
It is also sometimes used in the management of severe hypercalcemia in combination with adequate rehydration (Rossi, 2004).
Although disputed,[1] it is considered ototoxic: "usually with large parenteral doses and rapid administration and in renal impairment------------------------------------------------------------------------------
KCl Biological/Medical properties
Potassium is vital in the human body and oral potassium chloride is the common means to replenish it, although it can also be diluted and given intravenously. It can be used as a salt substitute for food, but due to its weak, bitter, unsalty flavor, it is usually mixed with regular salt, sodium chloride, for this purpose to improve the taste. Medically it is used in the treatment of hypokalemia and associated conditions, for digitalis poisoning, and as an electrolyte replenisher. Brand names include K-Dur®, Klor-Con®, Micro-K®, and Kaon Cl®. Side effects can include gastrointestinal discomfort including nausea and vomiting, diarrhea and bleeding of the gut. Overdoses cause hyperkalemia which can lead to paresthesia, cardiac conduction blocks, fibrillation and arrhythmias, also sclerotic.
------------------------------------------------------------------------------Atenolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. Introduced in 1976, atenolol was developed as a replacement for propranolol in the treatment of hypertension. Hypertension is a clinical condition in which the arterial blood pressure in rest exceeds constantly 140/90 mm Hg (as defined by the World Health Organization). Hypertension is a risk factor for stroke, myocardial infarction (heart attack), and serious renal damage.
Propranolol is known to readily cross the blood-brain barrier (BBB) and can pass into the brain, causing side-effects such as depression and nightmares; atenolol was specifically developed to be unable to pass through the blood-brain barrier in order to prevent this effect.
Contraindications
- bradycardia (pulse less than 50 bpm)
- cardiogenic shock
- asthma (may cause broncho-constriction)
- symptomatic hypotension (blood pressure of less than 100/60 mm Hg with dizziness, vertigo etc.)
- angina of the Prinzmetal type (vasospastic angina)
- metabolic acidosis (a severe condition with a more acid blood than normal)
- severe disorders in perpheral arterial circulation
- AV-Blockage of second and third degree (a particular form of arrhythmia)
- acutely decompensated congestive heart failure (symptoms may be fluid retention with peripheral edema and/or abdominal fluid retention (ascites), and/or lung edema)
- sick sinus syndrome (a particular form of arrhythmia, very rarely encountered)
- hypersensitivity and/or allergy to Atenolol
- Caution: patients with preexisting asthma bronchiale
- Caution: only if clearly needed during pregnancy, as atenolol may retard fetal growth and possibly causes other abnormalities. (If you are pregnant or plan to become pregnant, ask your doctor.)
[edit] Side effects
- See also: Propranolol
Atenolol causes significantly fewer central nervous system side effects (depressions, nightmares) and fewer bronchospastic reactions, both due to its particular pharmacologic profile.
It was the main beta-blocker identified as carrying a higher risk of provoking type 2 diabetes, leading to its downgrading in the United Kingdom in June 2006 to fourth-line agent in the management of hypertension.[1]
In addition, beta blockers blunt the usual sympathetic nervous system response to hypoglycemia (i.e. sweating, agitation, tachycardia). These drugs therefore have an ability to mask a dangerously low blood sugar, which further decreases their safety and utility in diabetic patients.
Dosage
In patients with normal renal function, the daily dose is 25 to 100 mg (in one dose or in two divided doses) depending on the indication and severity of the disease. In most patients, the physician will start with a low initial dose and make increments in weekly intervals as tolerated.
In patients with chronic heart failure the initial dose should be particularly low and increments should be made slowly.
In patients with a creatinin-clearance (an indicator for renal function) less than (35 ml/min) /1.73 m² the daily dose should be reduced to 25 to 50 mg daily according to the clinical response of the individual patient. If a patient with end-stage renal failure is scheduled on regular dialysis, usually 50 mg are given after each dialysis procedure. In these patients, a severe hypotension may occur afterwards.
[edit] Combination treatment of hypertension
If atenolol alone fails to control arterial hypertension, the drug can be combined with a diuretic and/or a vasodilator (hydralazine, or in severe cases minoxidil). Central alpha-agonists (e.g. clonidine), ACE Inhibitors or AT-Antagonists such as losartan can also be given additionally. Exert caution with calcium-antagonists of the verapamile-type as adjunct therapy because of additional negative impact on the muscular strength of the heart. Use of calcium-antagonists of the nifedipine-type is controversial.
[edit] Overdose
Symptoms of overdose are due to excessive pharmacodynamic actions on beta1 and also beta2-receptors. These include bradycardia, severe hypotension with shock, acute heart failure, hypoglycemia (= low blood sugar) and bronchospastic reactions. Treatment is largely symptomatic. Hospitalization and intensive monitoring is indicated. In early cases emesis can be induced. Activated charcoal is useful to absorb the drug. Atropine will counteract bradycardia, glucagon helps with hypoglycemia, dobutamine can be given against hypotension and the inhalation of a beta2-mimetic as hexoprenalin or salbutamol will terminate bronchospasms.
------------------------------------------------------------------------------Lisinopril (lye-SIN-o-pril, is a drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in treatment of hypertension, congestive heart failure, heart attacks and also in preventing renal and retinal complications of diabetes.
Pharmacology
Lisinopril is the lysine-analog of enalapril. Unlike other ACE inhibitors, lisinopril is not a prodrug and is excreted unchanged in the urine. In cases of overdosage, it can be removed from circulation by dialysis.
[edit] Clinical use
Its indications, contraindications and side effects are as those for all ACE inhibitors.
Its long half-life allows for once a day dosing which aids patient compliance. The usual daily dose in all indications ranges from 2.5mg in sensitive patients to 40mg. Some patients have been treated with 80mg daily and have tolerated this high dose well.
Lower dosages must be used in patients with higher grade renal impairment (glomerular filtration rate (GFR) lower than 30ml/min).
[edit] History/Brand Names
Lisinopril was developed by Merck & Co. and is marketed worldwide as Prinivil® and by AstraZeneca as Zestril®. In Australia it is marketed by AlphaPharm as Lisodur®.
------------------------------------------------------------------------------Dextropropoxyphene is an analgesic in the opioid category. It is used to treat mild to moderate pain and as an antitussive. It can be used to ease pain before, during and after an operation. It is often combined with acetaminophen in the preparation co-proxamol (Darvocet in the US and CAPADEX in AUS).
Analgesia
Dextropropoxyphene, like codeine, is a "weak" opioid. Codeine is more commonly used, however some individuals (approximately 10-20% of the Caucasian population) are unable to metabolize it, due to poor functioning of the enzyme CYP2D6. It is in these people that dextropropoxyphene is particularly useful, as its metabolism does not require CYP2D6.
-------------------------------------------------------------------------------Diazepam (IPA: [dʌɪˈazɪpam]), marketed under brand names Valium®, Stesolid, Diazemuls, Seduxen, Bosaurin, Diapam, Antenex and Apozepam)[1] is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, skeletal muscle relaxant and amnestic properties. This makes it a useful drug for treating anxiety, insomnia, seizures, alcohol withdrawal, and muscle spasms. It is also used before certain medical procedures (such as endoscopies) to reduce tension and anxiety, and in some surgical procedures to induce amnesia.[2][3]
Benzodiazepine
Diazepam is a benzodiazepine that binds to a specific subunit on the GABAA receptor at a site that is distinct from the endogenous GABA molecule.[5][6]The GABAA receptor is an inhibitory channel which, when activated, decreases neurologic activity.
Due to the role of diazepam as a positive allosteric modulator of GABA, when it binds to benzodiazepine receptors it causes inhibitory effects. This arises from the hyperpolarization of the postsynaptic membrane, due to the control exerted over negative chloride ions by GABAA receptors.[5][7]
Diazepam appears to act on areas of the limbic system, thalamus and hypothalamus, inducing anxiolytic effects. Its actions are due to the enhancement of GABA activity.[2][5]
Pharmacokinetics
Diazepam can be administered orally, intravenously, intramuscularly, or as a suppository.[13]
When diazepam is administered orally, it is rapidly absorbed and has a fast onset of action. The onset of action is 1-5 minutes for IV administration and 15-30 minutes for IM administration. The duration of the diazepam's main pharmacological effects is 15 minutes to 1 hour for both routes of administration.[14]
Peak plasma levels are achieved 30 minutes to 2 hours after oral administration. When diazepam is administered as an intramuscular injection, absorption is slow, erratic and incomplete.[1][15]
Diazepam is highly lipid-soluble, and is widely distributed throughout the body after administration. It easily crosses both the blood-brain barrier and the placenta, and is excreted into breast milk. After absorption, diazepam is redistributed into muscle and adipose tissue. Continual daily doses of diazepam will quickly build up to a high concentration in the body (mainly in adipose tissue), which will be far in excess of the actual dose for any given day.[13][15]
Diazepam is metabolised in the liver via the cytochrome P450 enzyme system. It has a biphasic half-life of 1-2 and 2-5 days, and has several pharmacologically active metabolites. The main active metabolite of diazepam is desmethyldiazepam (also known as nordazepam or nordiazepam). Diazepam's other active metabolites include temazepam and oxazepam. These metabolites are conjugated with glucuronide, and are excreted primarily in the urine. Because of these active metabolites, the serum values of diazepam alone are not useful in predicting the effects of the drug.[1][15]
Diazepam has a half-life (t1/2α) of 20-50 hours, and desmethyldiazepam has a half-life of 30-200 hours.[15]
Most of the drug is metabolised; very little diazepam is excreted unchanged.[13]
In humans, the protein binding of diazepam is around 98.5%.[1]
[edit] Indications
Diazepam is mainly used to treat anxiety, insomnia, and symptoms of acute alcohol or opiate withdrawal. It is also used as a premedication for inducing sedation, anxiolysis or amnesia prior to certain medical procedures (e.g. endoscopy).[1]
Diazepam is rarely used as a primary drug for the long-term treatment of epilepsy. This is due to the fact that tolerance to the anticonvulsant effects of diazepam usually develops within 6 to 12 months of treatment, effectively rendering it useless for this purpose.[13]
Diazepam has a broad spectrum of indications (most of which are off-label), including:
- Treatment of anxiety, panic attacks, and states of agitation[1]
- Treatment of status epilepticus, adjunctive treatment of other forms of epilepsy[1]
- Treatment of the symptoms of alcohol and opiate withdrawal[1]
- Initial management of mania, together with firstline drugs like lithium, valproate or other antipsychotics[citation needed]
- Adjunctive treatment (with antidepressants) of depression with symptoms of anxiety[citation needed]
- Adjunctive treatment (with antipsychotics), in patients who develop early extrapyramidal side-effects[citation needed]
- Adjunctive treatment of painful muscle conditions[11]
- Adjunctive treatment of spastic muscular paresis (para-/tetraplegia) caused by cerebral or spinal cord conditions such as stroke, multiple sclerosis, spinal cord injury (long-term treatment is coupled with other rehabilitative measures)[11]
- Palliative treatment of stiff person syndrome[7]
- Pre-/postoperative sedation, anxiolysis and/or amnesia (e.g. before endoscopic or surgical procedures)[11]
- Treatment of overdosage with hallucinogens or CNS stimulants[13]
- Adjunctive treatment of drug-induced seizures, resulting from exposure to sarin, VX, soman (or other organophosphate poisons; See CANA), lindane, chloroquine, physostigmine, or pyrethroids[13]
- Emergency treatment of eclampsia, along with IV magnesium sulfate
- Prophylactic treatment of oxygen toxicity during hyperbaric oxygen therapy.[17]
- Used in the treatment for irritable bowel syndrome. [18]
- Used to treat pain resulting from muscle spasms caused by various spastic dystonias, including blepharospasm, spasmodic dysphonia and Meige's Syndrome.
Side effects
Diazepam has a range of side effects which are common to most benzodiazepines. Most common side effects include:
- Somnolence
- Suppression of REM sleep or dreaming
- Impaired motor function
- Impaired coordination
- Impaired balance
- Dizziness
- Depression
- Anterograde amnesia (especially pronounced in higher doses)
- Reflex tachycardia[14]
Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties, including frequent urination and inability to control urination (urge incontinence), by decreasing muscle spasms of the bladder. It competitively antagonizes the M1, M2, and M3 subtypes of the muscarinic acetylcholine receptor. It also has direct spasmolytic effects on bladder smooth muscle as a calcium antagonist and local anesthetic, but at concentrations far above those used clinically. It is available orally in generic formulation and as the brand-names Ditropan® and Lyrinel XL®, and as a transdermal patch under the brand-name Oxytrol®.
Oxybutynin also shows promise for treatment of hyperhidrosis, or hyper-active sweating.
-------------------------------------------------------------------------------Paroxetine or paroxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRI) antidepressant. It was released in 1992 by the pharmaceutical company GlaxoSmithKline and has since become one of the most prescribed antidepressants on the market due to its apparent efficacy in treating depression as well as a spectrum of anxiety disorders ranging from panic attacks to phobias. The prescription of this drug is currently controversial because of legal proceedings against the manufacturer (see controversy below).
Approved
Paroxetine is primarily used to treat the symptoms of depression, obsessive-compulsive disorder (OCD), post-traumatic stress disorder (PTSD), panic disorder, generalized anxiety disorder (GAD), [1] social phobia/social anxiety disorder, [2] and premenstrual dysphoric disorder (PMDD).[3]
It was the first (and as of 2002, the only) antidepressant formally approved in the United States for the treatment of social anxiety disorder, causing it to be sometimes referred to (although inaccurately) as an anti-shyness drug.
------------------------------------------------------------------------------Aspirin or acetylsalicylic acid (acetosal) is a drug in the family of salicylates, often used as an analgesic (against minor pains and aches), antipyretic (against fever), and anti-inflammatory. It has also an antiplatelet (“blood-thinning”) effect and is used in long-term low-doses to prevent heart attacks and cancer.
Low-dose long-term aspirin irreversibly blocks the formation of thromboxane A2 in platelets, producing an inhibitory effect on platelet aggregation, and this blood-thinning property makes it useful for reducing the incidence of heart attacks. Aspirin produced for this purpose often comes in 75 or 81 mg dispersible tablets and is sometimes called “Junior aspirin” or “Baby aspirin.” High doses of aspirin are also given immediately after an acute heart attack. These doses may also inhibit the synthesis of prothrombin and may therefore produce a second and different anticoagulant effect.
Its primary undesirable side effects, especially in higher doses, are gastrointestinal distress (including ulcers and stomach bleeding) and tinnitus. Another side effect, due to its anticoagulant properties, is increased bleeding in menstruating women. Because there appears to be a connection between aspirin and Reye's syndrome, aspirin is no longer used to control flu-like symptoms or the symptoms of chickenpox in minors.[1]
Aspirin was the first discovered member of the class of drugs known as non-steroidal anti-inflammatory drugs (NSAIDs), not all of which are salicylates, though they all have similar effects and a similar action mechanism.
------------------------------------------------------------------------------Terazosin (Hytrin®) is a selective alpha 1 antagonist used for treatment of symptoms of prostate enlargement (BPH). It also acts to lower the blood pressure, so is a drug of choice for men with hypertension and prostate enlargement.
It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.
Most common side effects include dizziness, drowsiness, headache, constipation, loss of appetite, fatigue, nasal congestion or dry eyes, but they generally go away after only a few days of use. Sexual side effects are rare, but may include priapism or erectile dysfunction.
------------------------------------------------------------------------------Alendronate (Fosamax®, Merck) is a bisphosphonate drug used for osteoporosis and several other bone diseases. It is marketed alone as well as in combination with vitamin D (2,800 U, under the name Fosavance).
Pharmacology
Alendronate inhibits osteoclast-mediated bone-resorption. Like all bisphosphonates It is chemically related to inorganic pyrophosphate, the endogenous regulator of bone turnover. Whereas pyrophosphate and the first bisphosphonate, etidronate, are capable of inhibiting both osteoclastic bone resorption as well as the mineralization of the bone newly formed by osteoblasts, alendronate and the other potent N-containing bisphosphonates such as ibandronate and zoledronate specifically inhibit bone resorption without any effect on mineralization at pharmacalogically achievable doses. Its inhibition of bone-resorption is dose-dependent and approximately 1,000 times stronger than the equimolar effect of etidronate. Under therapy normal bone tissue develops, and alendronate is deposited in the bone-matrix in pharmacologically inactive form. For optimal action enough calcium and vitamin D are needed in the body in order to promote normal bone development. Hypocalcemia should therefore be corrected before starting therapy.
[edit] Uses
- Prophylaxis and treatment of female osteoporosis
- Treatment of male osteoporosis
- Prevention and treatment of corticosteroid-associated osteoporosis together with supplements of calcium and vitamin D
- Paget's disease
Donepezil, marketed under the trade name Aricept® (Eisai), is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. It has an oral bioavailability of 100% and easily crosses the blood-brain barrier. Because it has a half life of about 70 hours, it can be taken once a day. Initial dose is 5 mg per day, which can be increased to 10 mg per day after an adjustment period of at least 4 weeks.
Donepezil is sometimes used in combination with Memantine, a newer agent for Alzheimer's disease, as the response to both together is considered superior to donepezil alone. In moderate to severe Alzheimer's, a controlled clinical trial has shown that the addition of Memantine to stable donepezil therapy improves cognition, functioning and behavior.
Donepezil has been tested in other cognitive disorders including Lewy body dementia and Vascular dementia, but it is not currently approved for these indications. Donepezil has also been studied in patients with Mild Cognitive Impairment, schizophrenia, attention deficit disorder, post-coronary bypass cognitive impairment, cognitive impairment associated with multiple sclerosis, and Down syndrome. A 3 year NIH trial in patients with mild cognitive impairment reported that donepezil was superior to placebo in delaying rate of progression to dementia during the initial 18 months of the study but this was not sustained at 36 months. In a secondary analyses, a subgroup of individuals with the Apolipoprotein E4 genotype showed sustained benefits with donepezil throughout the study. However at this time donepezil is not indicated for prevention of dementia.
Donepezil is generally better tolerated than others in its class, simpler to use, and the agent with the most number of well controlled clinical trials. Common side effects include nausea, diarrhea, anorexia, abdominal pain, and vivid dreams. In 2006, Eisai, the manufacturer issued a statetment that a single vascular dementia study found a difference in the percent of study participants who died in the donepezil group (1.7%) versus the placebo group (0%) and that this could be due to an unusually low death rate on the placebo group. An analysis of all three Vascular Dementia trials, according to Eisai, "shows no statistically significant differences in observed mortality rates between the donepezil and placebo groups (1.7% vs. 1.1%)".
