Diphenhydramine chemical structure
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Diphenhydramine

Diphenhydramine hydrochloride (trade name Benadryl®, or Dimedrol outside the US) is an over-the-counter (OTC) antihistamine and sedative. It is also given in conjunction with typical antipsychotics to prevent akathisia. It is a member of the ethanolamine class of antihistaminergic agents. more...

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Diphenhydramine is widely used in nonprescription sleep aids (Nytol, Sominex, Unisom, Compoz, Excedrin PM, etc.) with a 50mg recommended dose mandated by the FDA. In the United Kingdom, Australia, New Zealand, South Africa, and other countries, a 50 to 100mg recommended dose is permitted. In spite of its use and effectiveness as a sleep-inducing agent, when this drug is sold as an antihistamine, warning of the potential loss of alertness is never prominently displayed on packaging, leading to unknown numbers of traffic fatalities.

Unlike true antihistamines, which prevent the release of histamine, diphenhydramine works by blocking the effect of histamine at H1 receptor sites. This results in effects such as the reduction of smooth muscle contraction, making diphenhydramine a popular choice for treatment of the symptoms of allergic rhinitis, hives, motion sickness, and insect bites and stings.

Diphenhydramine is a first generation antihistamine drug. Despite being one of the oldest antihistamines on the market, it is by and large the most effective antihistamine available, either by prescription or over-the-counter, and has been shown to exceed the effectiveness of even the latest prescription drugs. Consequently, it is frequently used when an allergic reaction requires fast, effective reversal of the (often dangerous) effects of a massive histamine release. However, it is not always the drug of choice for treating allergies. Like many other first generation antihistamines, is also a potent anticholinergic agent. This leads to profound drowsiness as a very common side-effect, along with the possibilities of motor impairment (ataxia), dry mouth and throat, flushed skin, rapid or irregular heartbeat (tachycardia), blurred vision at nearpoint due to lack of accommodation (cycloplegia), abnormal sensitivity to bright light (photophobia), pupil dilatation, urinary retention, constipation, difficulty concentrating, short-term memory loss, visual disturbances, hallucinations, confusion, and delirium.

In the 1960s it was found that diphenhydramine inhibits reuptake of the neurotransmitter serotonin. This discovery led to a search for viable antidepressants with similar structures and fewer side effects, culminating in the invention of fluoxetine (Prozac), a selective serotonin reuptake inhibitor (SSRI). A similar search had previously led to the synthesis of the first SSRI zimelidine from chlorpheniramine, also an antihistamine.

Recreational drug users sometimes take several times the recommended dose of diphenhydramine in order to attain an intense hallucinogenic (more accurately, delirious) state. Abusers often call diphenhyramine "The Pink Panther", in reference to the pink colored pills and syrups or they will say they are "drillin" or "Benatrippin" because of the common name brand, Benadryl®. The mental effects are described by many as "dreaming while awake" involving visual and auditory hallucinations which, unlike those experienced with most psychedelics, often cannot be readily distinguished from reality. Many users report a side effect profile consistent with tropane glycoalkaloidal poisoning. This is due to antagonism of muscarinic acetylcholine receptors in both the central and autonomic nervous system, inhibiting various signal transduction pathways. In the CNS, diphenhydramine readily crosses the blood-brain barrier, exerting effects within the visual and auditory cortex, accounting for reported visual and auditory disturbances. Other CNS effects occur within the limbic system and hippocampus, causing confusion and temporary amnesia. Toxicology also manifests in the autonomic nervous system, primarily at the neuromuscular junction, resulting in ataxia and extrapyramidal side-effects, and at sympathetic post-ganglionic junctions, causing urinary retention, pupil dialation, tachycardia, and dry skin & mucous membranes. Considerable overdosage can lead to myocardial infarction, serious ventricular dysrhythmias, coma and death. Such a side-effect profile is thought to give ethanolamine-class antihistamines a relatively low abuse liability.

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Get your summer on!
From Men's Fitness, 6/1/04 by Tamar Schreibman

SPF 55? CHECK. BlueBlocker clip-ons? Yup. Shamu inflatable lounge floater with beverage holder? Uh-huh. But are you up on the kindest way to slay a lobster? Or how to hit a wide-out in touch? Or how about the best strategies for having sex in the sand? Here, the buzz (see: "Bee stings") on all things Summer 2004.

Bee stings, treatment of

The first order of business is to remove the stinger, either with a pair of tweezers (preferably sterilized with a match) or your finger, or try scraping it off with the edge of a credit card, says Hilary L. Reich, M.D., a New York City-based dermatologist. If you experience shortness of breath or difficulty swallowing, call an ambulance--you might be having an allergic reaction. Otherwise, sterilize the area with soap and water, and apply antibiotic ointment.

Bike seat, height

Feel pain in your hip or thigh as you peddle? Make sure your bike seat is at the proper height. At the bottom of your pedal stroke, your leg shouldn't be perfectly straight; there should be a slight bend in the knee.

Bodysurf, how to

Maui's "first lady" of surfing, former world champion Nancy Emerson, has also been bodysurfing since age two. Her advice: Find a sandy shoreline ("Rocks hurt," she notes--but you already knew that), then swim to where the waves break. When you see a good rolling wave approaching, turn toward shore, get on your belly, and start swimming with your head up looking forward. Kick your legs to propel yourself (fins will give you great power and speed). Bring your arms to your sides as you ride the wave to reduce drag and hang loose--tensing up like a board adds 25 to 100 pounds of dead weight to your body.

Bug bites, treatment of

When a bug attacks this summer (and no doubt one will), reduce the itching and swelling with hydrocortisone 1% cream (available over the counter). Also, an oral anti-histamine like Benadryl (look for diphenhydramine on the label) can provide additional rapid relief. For mosquito bites, a lotion containing camphor and menthol will soothe the itch. For more painful fire-ant bites, go with a topical anesthetic like benzocaine 20%.

Burgers, how to grill

Bobby Flay, author of Boy Meets Grill, offers these suggestions:

1. Buy fresh, coarsely ground chuck. If flavor is top priority, don't get extra lean beef. Buffalo meat offers a beefy flavor with less fat.

2. Factor in shrinkage: "Meat shrinks due to loss of moisture and fat when being cooked," says Flay, who prefers the 80% lean variety. "That's just enough fat to keep the meat moist but not so much that your burger disappears on the grill." Generally use about five ounces of meat for each patty.

3. As you form patties, add a coarse salt like kosher and grind on fresh black pepper. "Pre-ground doesn't have the vibrancy of flavor."

4. Cook on high heat: four minutes on each side for medium-rare, five minutes for medium, and six minutes for well-done.

Dog, care of

Where you go, the dog goes, right? But your best friend doesn't fare as well in the heat as you do. Annemarie Lucas of the Animal Planet network's Animal Precinct suggests shaving your dog's hair to one-inch length to prevent overheating; completely shaving him down will rob him of sun protection altogether (and make him look pretty goofy). At the beach, limit his time in the surf. Not only will saltwater irritate his skin, but it'll also dehydrate him quicker if he drinks enough of it.

Exercise outdoors, best time to

Schedule that pick-up game or bike trek for early morning or late afternoon. You will fatigue faster between 11 a.m. and 2 p.m, when the sun is at its peak. Midday activity also puts you at risk for dehydration and heatstroke.

Flings, rules for summer

The key to keeping a summer affair just an affair is to limit the amount of time you spend alone with the woman, says Rick Solomon, fledgling porn auteur and co-star of The Paris Hilton Sex Tape. "It's tough for her to tell you those three scary words--'I love you'--if you're constantly surrounded by your buddies, loud music, and an open bar." Solomon also suggests withholding your true intentions until Labor Day. "It doesn't matter how liberated she thinks she is. No woman just wants to be some guy's summer fling."

Haircut, best summer "The harsh look is out," says Losi of New York City's John Frieda Salon, who's styled the hair of Mark Ruffalo, Jake Gyllenhaal, and Luke Wilson. For summer, Losi suggests growing your hair, especially your bangs, below your nose, then tucking it behind your ears. Can't go long-haired at work? Try what Losi calls "mussed," which means cutting your hair about two inches all over, then running hair paste through to spike it up or push to the side for work.

Hangovers, prevention of

If you drink at the beach, you'll feel pretty bad once the buzz wears off, since both alcohol and the sun leave you dehydrated. The best way to prevent a wicked summer hangover is to drink water before, during, and after you imbibe, or roughly one glass of water for every drink.

Health half-myths, debunking of

It's dangerous to swim too soon after eating: Although you're more likely to get a muscle cramp, or side stitch, in your diaphragm if you swim right after downing a burger, it's more bothersome than dangerous, says Jane Katz, Ed.D., author of Swimming for Total Fitness. A cramp can develop when you exercise muscles deprived of blood-rich oxygen that is being used in digestion. It takes nearly four hours for food to be fully digested, but holding off on those laps for an hour after eating can only help.

You're most likely to get a sunburn on hazy days: Mom was right, but for the wrong reason, says James Spencer, M.D., director of dermatological surgery at New York City's Mount Sinai School of Medicine. It's not that the sun is stronger on cloudy days than on sunnier ones; it's that the clouds block visible sun rays, fooling you into thinking there aren't many harmful (and invisible) UV rays. Actually, they pass right through the cirrus, so you still need to wear your sunblock.

Jellyfish stings, treatment of

Remove any tentacles, which contain stinging cells, with tweezers or a stick. Contrary to popular belief, urine can actually jump-start the stinging cells. Instead, rinse the area with saltwater--freshwater will activate the jellyfish venom, leaving you in even more pain. Finally, pop some Advil or Tylenol and stay still; moving the area can spread the venom.

Lobster, most humane way to cook

It's generally agreed that a lobster's nervous system is too primitive to feel pain, but for sensitive types, that doesn't make boiling one alive any easier. The solution: Place your live lobster in the freezer for 15 to 20 minutes before boiling. Once numb, it'll thrash less in the pot.

Mojito, the new For the past few years, the mojito has reigned as the cocktail of summer; even Pierce Brosnan's James Bond chose one over his usual martini in 2002's Die Another Day. This year, consider the MoFo, a smoother version of the minty Cuban drink, concocted exclusively for MF by Luigi Valenciana of Seattle's Mojito Cafe.

To get your own MoFo working, here's what you'll need:

Poisonous plants, treating exposure to

Poison ivy and its cousins poison oak and poison sumac release a potent toxin called urushiol oil--just one-billionth of a gram of it on your skin can cause a nasty rash. If you've been exposed to one of the plants, treat the area immediately with rubbing alcohol; this may not stop an outbreak, but it will keep it from spreading.

Pump, how to get a quick

To hit the beach with that just-back-from-the-gym look, you need some quick pumpitude. And since the pump phenomenon requires forcing blood into the muscles faster than it can be carried out, ladder reps--performing 5-10 reps for every quarter of the range of motion--are perfect. For chest, do ladder push-ups: 5-10 reps from the floor to a quarter of the way up, 5-10 from a quarter of the way to halfway up, 5-10 from a quarter of the way to three-quarters, and finally, 5-10 full-range reps. Use the same technique with dumbbells for presses, lateral raises, or curls. With your muscles bursting, you're now ready to go and kick some sand.

Run on beach, when to

That soft, forgiving sand by the shore might seem like an inviting jogging track, but it "puts strain on your Achilles tendon and the muscles that support your arch," says Richard Braver, M.D., a New Jersey sports podiatrist. Instead, run on the beach at low tide: When the shoreline recedes, it leaves hard, packed sand in its wake, which provides a much firmer running surface.

Shirts, taking off of?

Going shirtless in the summer is one of our inalienable rights, but some days are better than others to play skins. On a bright sunny day with dry heat, you'll be cooler playing hoops or jogging with a shirt, since you won't absorb as many of the sun's rays, says Larry Kenney, Ph.D., president of the American College of Sports Medicine. Lose the shirt on humid, overcast days, when the sun isn't as strong.

Shoes without socks

Casual shoes without socks are OK. Dress shoes without socks? Not OK.

Skim a rock, how to

An in-depth study conducted by a team of French researchers discovered that the key to successful rock skimming is ... a flat, round rock. OK, they also learned valuable stuff: When chucking the rock, keep the throwing hand back, hold the stone between your thumb and forefinger, and angle your hand 20 degrees to the water, says Christophe Clanet, who led the research team. Remember, you're going for spin, which creates the bounce, so let the stone roll off the forefinger. Because you don't want to break the water's surface, flick the wrist. Once you hit 39 skips, call us--the current record is 38.

Summer Fridays, instituting

How can you steer your corporate ship toward Summer Fridays? "You really can't," says Fortune columnist Stanley Bing, author of What Would Machiavelli Do? "You'll make a name for yourself as a slacker and goof-off, and will then have a harder time slacking and goofing off." Bing's solution: Use legitimate Friday vacation days for buy-some, get-some free. "Spread four Fridays off over 10 weeks, and no one will notice you've actually taken five. Just send out a note saying, 'I'm going to be taking Fridays off. I'm not sure which ones, but if I'm not here on a Friday ...' If you've rented a house, add, 'We're having a BBQ in July and want you to come.' Obviously, no one will."

Sunglasses, choosing

You don't wear the same sneakers playing basketball that you do playing softball. The same should go for your sunglasses. For driving, a pair with brown- or copper-tinted lenses will improve contrast. For water sports, glasses with double-gradient lenses, which are darker on the top and bottom and lighter in the middle, block water reflection. And for games on the sand and on the court, get polarized lenses, which cut reflected glare.

Work, getting time off

You've already burned through your vacation allowance. But today, Al Roker says it will be 82 and sun-drenched at the shore. How to escape? "Better to beg forgiveness than ask permission," recommends Fortune's Stanley Bing. "If someone says, 'Where were you Tuesday?' Say, 'Oh, I'm sorry ... I'm ... you know ... so sorry.' That's better than asking for that day off and having your boss say, 'No. In fact, let's have our staff meeting Tuesday.'" Just use sparingly: People can smell an Omarosa pretty fast.

Touch football, best play in

No helmet and pads doesn't mean no strategy. Here's an ideal play for eight-on-eight--the standard flag-football team size--that gets yardage every time. For the spread-formation four-man hook," explains Michael Cihon, United States Flag and Touch Football League executive director, you have a "wide out" on each side, 15 yards off-center, and a "slot" receiver on each side, eight-yards off-center. With the quarterback in shotgun, receivers run five to 10 yards up field, then cut back two yards. Because defenders play behind receivers, the QB can hit an open man.

Water in your ear, removal of

Grab hold of a wall or fence with the arm on the same side of your body as the water-clogged ear. Stand on the leg of the same side and tilt your ear toward your shoulder. Hop up and down, until the water drains out.

Wine, anti-snob summer

In the U.S., sweet rose is considered the Schlitz of summer wines. But in Europe, winemakers turn out a dry version that tastes more like berries. Now U.S. vintners are producing a Euro-style rose that goes great at the beach. Brad Hickey, wine director at NYC's Bouley, suggests Bonny Doon Vin Gris de Cigare ($11) from California. And let the snobs scoff.

Women at the beach, how to meet

Sometimes the cliches work. After surveying Orange County, Calif., surfers, who exhibit uncanny skill in this department, we learned that the surest way to meet women on the beach is to ask for sunblock. "Don't ask them to put it on you--that's creepy, dude," says Mike Shaon, manager of an O.C. surf shop. "Three out of four times, it'll lead to a conversation and maybe some beers later." Not to mention how women are impressed by conscientious types. "They know you're taking care of your skin."

Calories Burned

Calculations for a 180-pound man, doing each for one hour:

Scuba or skin diving: 605

Caddying: 475

Pushing a lawn mower: 475

Washing your car: 368

Frisbee: 259

Playing guitar, seated: 164

Sex, vigorous: 123

Reclining on a lawn chair: 82

Drinking beer, slowly: 81

Lying in sun: 65

Beach campfire, how to build

Claim some open space (clear of fire hazards) and dig down a foot. Criss-cross flat rows of solid timber, or driftwood in a square shape, about two feet by two feet. After you've built it up two feet high, top off your pile with tinder, small twigs, or shredded rope, instructs Eagle Scout David Srebro, a camping director for the Boy Scouts of America. You're lighting from the top down, so make sure your fixings will catch. And don't add more wood too quickly; wait till the first batch burns down to the hot-ember stage, then s'more out!

Junk food calorie count:

CORN DOG

250 calories

21 g carbs

COTTON CANDY

370 calories

92.5 g carbs

FUNNEL CAKE

380 calories

85 g carbs

SMALL LOADED NACHOS

(cheese, beans, ground beef, peppers)

569 calories

56 g carbs

Cannonball dive, the perfect

It doesn't matter if you're not built like an actual cannonball; although "a good carbo-load the night before would definitely help," notes Steve McFarland, executive director of this June's U.S. Olympic team diving trials. Whether from a diving board or a dock, jump straight up, tuck your knees into your chest, and grab hold of your legs with both arms. Keep clutching your knees until you're completely submerged--you're not going for a massive splash, just a high one. (Think huge fountain stream.)

Sex outdoors

Sex on the beach: It's not just a fruity tourist drink. Although even the biggest beach towel can't prevent sand from getting in your crevices (or hers), here are guidelines from Lou Paget, author of 365 Days of Sensational Sex, for making it great in the great outdoors:

1. Genitals can burn, so cover them in sunscreen--but not your penis; it can irritate her insides.

2. All 50 states have laws against indecent exposure and public lewdness, acts in which you expose your nether regions to others.

3. Ideally, she should already apply a water-based lubricant inside of her before you hit the ocean. Your best position is standing up, with her legs wrapped around your waist. This way you can disengage quickly before getting caught.

Grill burn, treatment of accidental

So you had a few too many and, confusing your hand for a meat patty, you slapped it on a flaming grill. Dumb? Yes. Serious? Probably not. First, run cold water on the burn until the throbbing stops, and then wash with mild soap and water. After applying topical antibacterial ointment, cover the burn with a band-aid or non-adhesive dressing. Blisters might form, but don't open them; they act as a natural barrier against infection causing microorganisms.

Sharks, why you shouldn't fear

Sure, sharks are in the ocean, but that doesn't mean you should stay out of it. According to George Parsons, a director at Chicago's Shedd Aquarium, sharks kill an average of only eight people worldwide each year. More people died from tipped vending machines last year than they did from shark attacks. Plus, sharks don't even like the taste of human blood. Usually they let go after just one bite.

COPYRIGHT 2004 Weider Publications
COPYRIGHT 2004 Gale Group

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